International Journal of Management Research and Emerging Sciences
Proficient working capital administration is getting significant for café firms adapting to frail... more Proficient working capital administration is getting significant for café firms adapting to frail money related conditions and expanded monetary vulnerability. The study is coordinated on the basis of information of 56 firms in Pakistan gathered over the period of 10 years 2009-2018 to discover the relationship of holding excess cash and firm’s performance in the presence of financial constraints. Two speculations were created for examination, how abundance money holding impact venture and furthermore to inspect the association under the moderation role of financial constraints. Holding of excess cash, income, market to book proportion were taken as self-ruling elements while adventure of complete assets, return on value, return on resources and influence were taken as dependent components and money related necessities, for instance, liquidity was taken as coordinating variable while firm age, firm size and benefit were taken as control factors. The first outcome was that we recogni...
La presente invention concerne une forme cristalline (B) d'acetate de methyle de {(1R,2S,3S,4... more La presente invention concerne une forme cristalline (B) d'acetate de methyle de {(1R,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxybenzylphenyl]-2,3,4-trihydroxy-6,8-dioxabicyclo [3.2. 1]oct-1-yle} de formule (II) et son procede de preparation. La presente invention concerne egalement un procede de conversion d'une forme cristalline (B) d'acetate de methyle de {(1 R,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-2,3,4-trihydroxy-6,8-dioxabicyclo[3.2.1]oct-1-yle} de formule (II) en Ertugliflozin.
Journal of Accounting and Finance in Emerging Economies, 2020
Detachement of business practicess and ethics led to a number of business scandals and unethical ... more Detachement of business practicess and ethics led to a number of business scandals and unethical practices in workplaces. This urged scholars and practioners to investigate importance of morality at workplace. This study has highlighted the role of ethical leaders in shaping whistleblowing intentions of their subordinates. Moreover, this study has also investiagted the role of moral identity. A total of four hypotheses, examining the direct effect of ethical leadership on moral identity and whistleblowing intentions and the mediationing role of moral identity were proposeed. This study adopted a timelagged study design and collected information from employee-peer dyads at three points in time. Data was gathered from 214 employees working in service sector. Results verified the role of ethical leaders in shaping moral identity of employees as well as their whistleblowing intentions. Alongwith, the findings also suggest that moral identity acts as an intervening mechanism between ethi...
Original Scientific Research Papers (Full articles and short notes) and Review articles are invit... more Original Scientific Research Papers (Full articles and short notes) and Review articles are invited for the coming issues of Pakistan Journal of Agricultural Research
In this era of internet, E-Business and e-commerce applications are using Databases as their inte... more In this era of internet, E-Business and e-commerce applications are using Databases as their integral part. These Databases irrespective of the technology used are vulnerable to SQL injection attacks. These Attacks are considered very dangerous as well as very easy to use for attackers and intruders. In this paper, we are proposing a new approach to detect intrusion from attackers by using SQL injection. The main idea of our proposed solution is to create trusted user profiles fetched from the Queries submitted by authorized users by using association rules. After that we will use a hybrid (anomaly + misuse) detection model which will depend on data mining techniques to detect queries that deviates from our normal behavior profile. The normal behavior profile will be created in XML format. In this way we can minimize false positive alarms.
In the present investigation, a series of 2-[2-(aryl)-2-oxo-ethylsulfanyl]-3-(aryl/propyl)-3H-qui... more In the present investigation, a series of 2-[2-(aryl)-2-oxo-ethylsulfanyl]-3-(aryl/propyl)-3H-quinazolin-4-ones have been synthesized and tested for their potential against seizures in mice. All the newly synthesized compounds show moderate to high protection against 6 Hz partial seizure with compound 2b, 2-(2-oxo-2-p-tolyl-ethylsulfanyl)-3-phenyl-3Hquinazolin-4-one emerging as the most active anticonvulsant agent endowed with neuroprotective effect against NMDA and kainate induced excitotoxicity. The results of whole brain GABA assay indicates that the seizure protective activity of 2b can be either due to the increased brain GABA level or due to neuroprotective action.
La presente invention porte sur le mirabegron, dimethyl-sulfoxyde, sur des procedes pour le prepa... more La presente invention porte sur le mirabegron, dimethyl-sulfoxyde, sur des procedes pour le preparer, sur une composition pharmaceutique le contenant, et sur son utilisation pour le traitement de l'hyperactivite vesicale. La presente invention concerne egalement des procedes de preparation de mirabegron a partir de solvate mirabegron dimethyl-sulfoxyde.
This paper describes an in depth analysis of successful and unsuccessful software Projects and th... more This paper describes an in depth analysis of successful and unsuccessful software Projects and the Role of Software Project Mangers in that success. One of the main reason in software project success is manager. Software houses are investing too much in this regard but the average ratio of software project failure is on the high side. Project managers experience, technical knowledge, and skills are not good enough for success in general. In this paper we have conducted a survey related to the approached used by different project managers, their methods and techniques, and the success ratio of their projects, and the steps they took during their projects. We will explore the core reasons of software project success and then will suggest key steps to be taken by the software project managers to deliver a successful software project.
Social media has revolutionalised the ways of communication and sharing information and interests... more Social media has revolutionalised the ways of communication and sharing information and interests. The rapid growth of social media and social networking sites, especially, in developing country like India is providing marketer a new avenue to contact customers. Though, organizations are increasing their spend in social media, it is difficult to measure a real return on investment. This paper attempts to assess the impact of usage of social media on purchase decision process. The paper examines the usage pattern and its influences the five stages of purchase process. The study finds that the social media is most widely used in information source for perceived convenience, effectiveness and perceived credibility. Also, the social media reviews and opinions affect the purchase decision process; however, tendency of share their experiences post purchase is surprisingly low.
In this paper, synthesis, single-crystal X-ray structure, Hirshfeld and DFT studies of 1,8-dichlo... more In this paper, synthesis, single-crystal X-ray structure, Hirshfeld and DFT studies of 1,8-dichloro-9,10-dihydro-9,10-ethanoanthracene-11-carboxylic acid are discussed. Different intermolecular contacts affecting the crystal stability are studied using Hirshfeld calculations. The H…Cl and O…H contacts are the most significant, showing corresponding interaction distances of 2.731 Å (Cl2…H10) and 1.681Å (H1…O1), 2.328 Å (O1…H13), 2.510 Å (O1…H12) based on Hirshfeld calculations. DFT calculations are carried out to study the electronic behavior, as well as the 1H- and 13C-NMR spectra of the synthesized compound. The computed NMR chemical shifts show excellent correlation with the experimental data (R2 = 0.9884–0.9705).
Fresh and clean water is consistently depleting and becoming a serious problem with rapid increas... more Fresh and clean water is consistently depleting and becoming a serious problem with rapid increases in population, so seawater desalination technology has captured global attention. For an efficient desalination process, this work proposes a novel, nanofibrous, thin-film composite membrane (NF-TFC) based on the deposition of the nanofibrous active layer of a blend of chitosan (CS) and poly (vinylpyrrolidone) (PVP) crosslinked with maleic acid on a 3-triethoxysilylpropylamine functionalized cellulose acetate substrate. FTIR analysis demonstrated the development of chemical and physical interactions and confirmed the incorporation of functional groups present in the NF-TFC. Scanning electron microscopy (SEM) micrographs depict the fibrous structure of the active layers. The reverse osmosis (RO) desalination characteristics of NF-TFC membranes are elevated by increasing the concentration of the crosslinker in a CS/PVP blend. Cellulose acetate (CA)-S4 attained an optimal salt rejection ...
Pure water is becoming less available with increases in world population, so seawater desalinatio... more Pure water is becoming less available with increases in world population, so seawater desalination is becoming more important. For efficient seawater desalination, this paper proposes a novel mixed matrix membrane (MMM) based on the deposition of a poly(vinyl alcohol) (PVA) nanofibrous active layer on a 3-triethoxysilylpropylamine-functionalized cellulose acetate substrate. The active layer is fabricated by utilizing a tetraethyl orthosilicate-crosslinked PVA incorporating zinc oxide nanoparticles (ZnO-NPs) and sodium alginate (NaAlg). The overall reverse osmosis performance of the MMMs is enhanced by the infusion of ZnO-NPs and NaAlg in PVA; we find the optimum concentration for the best performance to be ZnO-NPs at 0.1 wt % and NaAlg at 0.01 wt %. In terms of permeation flux, salt rejection, salt passage, stability, long-term rejection, membrane antifouling, reusability, and chlorine resistance, the proposed MMMs are examined using a dead-end reverse osmosis filtration setup. The results show that the active layer achieves an optimal permeation flux of 34.6 L/m 2 h, a natural sea salt rejection of 97%, and a chlorine resistance of 93%, suggesting that the proposed MMMs can be useful for seawater desalination.
Depravity of malaria in terms of morbidity and mortality in human beings makes it a major health ... more Depravity of malaria in terms of morbidity and mortality in human beings makes it a major health issue in tropical and subtropical areas of the globe. Drug counterfeiting and non-adherence to the treatment regimen have significantly contributed to development and spread of multidrug resistance that has highlighted the need for development of novel and more efficient antimalarial drugs. Complexity associated with cancer disease and prevalence of diversified cell populations vindicates highly specific treatment options for treatment of cancer. Resistance to these anticancer agents has posed a great hindrance in successful treatment of cancer. Pondering this ongoing situation, it was speculated to develop novel compounds targeting malaria and cancer. Moving on the same aisle, we synthesized pyrazole acrylic acid based oxadiazole and amide derivatives using multi-step reaction pathways (6a-x; 6a'-h'). Schizont maturation inhibition assay was employed to determine antimalarial po...
This work is concerned with the modelling of the interaction of fluid flow with flexibly supporte... more This work is concerned with the modelling of the interaction of fluid flow with flexibly supported rigid bodies. The fluid flow is modelled by Lattice-Boltzmann Method, coupled to a set of ordinary differential equations describing the dynamics of the solid body in terms its elastic and damping properties. The time discretization of the body dynamics is performed via the Time Discontinuous Galerkin Method. Several numerical examples are presented and highlight the robustness and efficiency of the proposed methodology, by means of comparisons with previously published results. The examples show that the present fluid-structure method is able to capture vortexinduced oscillations of flexibly-supported rigid body.
New hydrazone incorporated triazines were designed and synthesized using an appropriate synthetic... more New hydrazone incorporated triazines were designed and synthesized using an appropriate synthetic route with regard to essential pharmacophores, and evaluated for their anticonvulsant activity through maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole-induced seizure (scPTZ) screenings. Among the tested compounds, 4-[{2-(5-(3-chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6k (MES ED50 54.31, scPTZ ED50 92.01) and 4-[{2-(5-(4-chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6r (MES ED50 46.05, scPTZ ED50 83.90) emerged as the most active anticonvulsant agents having GABAergic effects. Compounds 6k and 6r also showed lesser CNS depressant effect than the standard drug carbamazepine. To obtain further insights into the binding interactions of these molecules, molecular docking studies were carried out.
Abstract: Several 3-chloro-4-flourophenyl substituted semicarbazones have been synthesized in thr... more Abstract: Several 3-chloro-4-flourophenyl substituted semicarbazones have been synthesized in three steps involving aryl urea and aryl semicarbazide formation. The structures have been confirmed by spectral and elemental analyses. Some selected ...
Abstract A new series of N-(6-chlorobenzothiazol-2-yl)-2-substituted-acetamides (3ah) and N-(6-c... more Abstract A new series of N-(6-chlorobenzothiazol-2-yl)-2-substituted-acetamides (3ah) and N-(6-chlorobenzothiazol-2-yl)-2-(substituted-benzylidene) hydrazinecarbothioamides (5ah) were synthesized and characterized by IR, 1 H NMR, mass and elemental analysis. In vivo ...
In order to produce new lead for an xio lytic and antidepressant drug, a new series of quinazolin... more In order to produce new lead for an xio lytic and antidepressant drug, a new series of quinazoline analogues was designed to mimic ATC-0175 structural features and fitted with functional groups believed to enhance an xio lytic and antidepressant activity. The synthesized co mpounds were evaluated for an xiolytic and antidepressant activity by elevated plus-maze and tail-suspension method. The targeted compounds (SKF 1-15) were synthesized fro m 2-chlo ro-6,7-dimetho xy quinazolin-4-amine and N-(substituted benzyl) propan-1-amines in isoamy l alcohol med iu m under reflu x for 24 h. A ll the targeted compounds are new chemical entit ies and obtained in satisfactory yields (Table 1). The structures of synthesized compounds are in good agreement with their corresponding spectral data.
A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synt... more A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synthetic route and characterized by spectral analysis (IR, 1H NMR, 13C NMR and Mass). The anticonvulsant activity of the synthesized compounds was determined using doses of 30, 100, and 300 mg kg-1 against maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Six compounds exhibited protection in both models and 2-(1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene)-N-p-tolylsemicarbazone emerged as the most active compound of the series without any neurotoxicity and significant CNS depressant effect. Liver enzyme estimations (SGOT, SGPT, Alkaline phosphatase) of the compound also showed no significant change in the enzymes levels. Moreover, it caused 80% elevation of γ-amino butyric acid (GABA) levels in the whole mice brain, thus indicating that it could be a promising candidate in designing of a potent anticonvulsant drug.
International Journal of Management Research and Emerging Sciences
Proficient working capital administration is getting significant for café firms adapting to frail... more Proficient working capital administration is getting significant for café firms adapting to frail money related conditions and expanded monetary vulnerability. The study is coordinated on the basis of information of 56 firms in Pakistan gathered over the period of 10 years 2009-2018 to discover the relationship of holding excess cash and firm’s performance in the presence of financial constraints. Two speculations were created for examination, how abundance money holding impact venture and furthermore to inspect the association under the moderation role of financial constraints. Holding of excess cash, income, market to book proportion were taken as self-ruling elements while adventure of complete assets, return on value, return on resources and influence were taken as dependent components and money related necessities, for instance, liquidity was taken as coordinating variable while firm age, firm size and benefit were taken as control factors. The first outcome was that we recogni...
La presente invention concerne une forme cristalline (B) d'acetate de methyle de {(1R,2S,3S,4... more La presente invention concerne une forme cristalline (B) d'acetate de methyle de {(1R,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxybenzylphenyl]-2,3,4-trihydroxy-6,8-dioxabicyclo [3.2. 1]oct-1-yle} de formule (II) et son procede de preparation. La presente invention concerne egalement un procede de conversion d'une forme cristalline (B) d'acetate de methyle de {(1 R,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-2,3,4-trihydroxy-6,8-dioxabicyclo[3.2.1]oct-1-yle} de formule (II) en Ertugliflozin.
Journal of Accounting and Finance in Emerging Economies, 2020
Detachement of business practicess and ethics led to a number of business scandals and unethical ... more Detachement of business practicess and ethics led to a number of business scandals and unethical practices in workplaces. This urged scholars and practioners to investigate importance of morality at workplace. This study has highlighted the role of ethical leaders in shaping whistleblowing intentions of their subordinates. Moreover, this study has also investiagted the role of moral identity. A total of four hypotheses, examining the direct effect of ethical leadership on moral identity and whistleblowing intentions and the mediationing role of moral identity were proposeed. This study adopted a timelagged study design and collected information from employee-peer dyads at three points in time. Data was gathered from 214 employees working in service sector. Results verified the role of ethical leaders in shaping moral identity of employees as well as their whistleblowing intentions. Alongwith, the findings also suggest that moral identity acts as an intervening mechanism between ethi...
Original Scientific Research Papers (Full articles and short notes) and Review articles are invit... more Original Scientific Research Papers (Full articles and short notes) and Review articles are invited for the coming issues of Pakistan Journal of Agricultural Research
In this era of internet, E-Business and e-commerce applications are using Databases as their inte... more In this era of internet, E-Business and e-commerce applications are using Databases as their integral part. These Databases irrespective of the technology used are vulnerable to SQL injection attacks. These Attacks are considered very dangerous as well as very easy to use for attackers and intruders. In this paper, we are proposing a new approach to detect intrusion from attackers by using SQL injection. The main idea of our proposed solution is to create trusted user profiles fetched from the Queries submitted by authorized users by using association rules. After that we will use a hybrid (anomaly + misuse) detection model which will depend on data mining techniques to detect queries that deviates from our normal behavior profile. The normal behavior profile will be created in XML format. In this way we can minimize false positive alarms.
In the present investigation, a series of 2-[2-(aryl)-2-oxo-ethylsulfanyl]-3-(aryl/propyl)-3H-qui... more In the present investigation, a series of 2-[2-(aryl)-2-oxo-ethylsulfanyl]-3-(aryl/propyl)-3H-quinazolin-4-ones have been synthesized and tested for their potential against seizures in mice. All the newly synthesized compounds show moderate to high protection against 6 Hz partial seizure with compound 2b, 2-(2-oxo-2-p-tolyl-ethylsulfanyl)-3-phenyl-3Hquinazolin-4-one emerging as the most active anticonvulsant agent endowed with neuroprotective effect against NMDA and kainate induced excitotoxicity. The results of whole brain GABA assay indicates that the seizure protective activity of 2b can be either due to the increased brain GABA level or due to neuroprotective action.
La presente invention porte sur le mirabegron, dimethyl-sulfoxyde, sur des procedes pour le prepa... more La presente invention porte sur le mirabegron, dimethyl-sulfoxyde, sur des procedes pour le preparer, sur une composition pharmaceutique le contenant, et sur son utilisation pour le traitement de l'hyperactivite vesicale. La presente invention concerne egalement des procedes de preparation de mirabegron a partir de solvate mirabegron dimethyl-sulfoxyde.
This paper describes an in depth analysis of successful and unsuccessful software Projects and th... more This paper describes an in depth analysis of successful and unsuccessful software Projects and the Role of Software Project Mangers in that success. One of the main reason in software project success is manager. Software houses are investing too much in this regard but the average ratio of software project failure is on the high side. Project managers experience, technical knowledge, and skills are not good enough for success in general. In this paper we have conducted a survey related to the approached used by different project managers, their methods and techniques, and the success ratio of their projects, and the steps they took during their projects. We will explore the core reasons of software project success and then will suggest key steps to be taken by the software project managers to deliver a successful software project.
Social media has revolutionalised the ways of communication and sharing information and interests... more Social media has revolutionalised the ways of communication and sharing information and interests. The rapid growth of social media and social networking sites, especially, in developing country like India is providing marketer a new avenue to contact customers. Though, organizations are increasing their spend in social media, it is difficult to measure a real return on investment. This paper attempts to assess the impact of usage of social media on purchase decision process. The paper examines the usage pattern and its influences the five stages of purchase process. The study finds that the social media is most widely used in information source for perceived convenience, effectiveness and perceived credibility. Also, the social media reviews and opinions affect the purchase decision process; however, tendency of share their experiences post purchase is surprisingly low.
In this paper, synthesis, single-crystal X-ray structure, Hirshfeld and DFT studies of 1,8-dichlo... more In this paper, synthesis, single-crystal X-ray structure, Hirshfeld and DFT studies of 1,8-dichloro-9,10-dihydro-9,10-ethanoanthracene-11-carboxylic acid are discussed. Different intermolecular contacts affecting the crystal stability are studied using Hirshfeld calculations. The H…Cl and O…H contacts are the most significant, showing corresponding interaction distances of 2.731 Å (Cl2…H10) and 1.681Å (H1…O1), 2.328 Å (O1…H13), 2.510 Å (O1…H12) based on Hirshfeld calculations. DFT calculations are carried out to study the electronic behavior, as well as the 1H- and 13C-NMR spectra of the synthesized compound. The computed NMR chemical shifts show excellent correlation with the experimental data (R2 = 0.9884–0.9705).
Fresh and clean water is consistently depleting and becoming a serious problem with rapid increas... more Fresh and clean water is consistently depleting and becoming a serious problem with rapid increases in population, so seawater desalination technology has captured global attention. For an efficient desalination process, this work proposes a novel, nanofibrous, thin-film composite membrane (NF-TFC) based on the deposition of the nanofibrous active layer of a blend of chitosan (CS) and poly (vinylpyrrolidone) (PVP) crosslinked with maleic acid on a 3-triethoxysilylpropylamine functionalized cellulose acetate substrate. FTIR analysis demonstrated the development of chemical and physical interactions and confirmed the incorporation of functional groups present in the NF-TFC. Scanning electron microscopy (SEM) micrographs depict the fibrous structure of the active layers. The reverse osmosis (RO) desalination characteristics of NF-TFC membranes are elevated by increasing the concentration of the crosslinker in a CS/PVP blend. Cellulose acetate (CA)-S4 attained an optimal salt rejection ...
Pure water is becoming less available with increases in world population, so seawater desalinatio... more Pure water is becoming less available with increases in world population, so seawater desalination is becoming more important. For efficient seawater desalination, this paper proposes a novel mixed matrix membrane (MMM) based on the deposition of a poly(vinyl alcohol) (PVA) nanofibrous active layer on a 3-triethoxysilylpropylamine-functionalized cellulose acetate substrate. The active layer is fabricated by utilizing a tetraethyl orthosilicate-crosslinked PVA incorporating zinc oxide nanoparticles (ZnO-NPs) and sodium alginate (NaAlg). The overall reverse osmosis performance of the MMMs is enhanced by the infusion of ZnO-NPs and NaAlg in PVA; we find the optimum concentration for the best performance to be ZnO-NPs at 0.1 wt % and NaAlg at 0.01 wt %. In terms of permeation flux, salt rejection, salt passage, stability, long-term rejection, membrane antifouling, reusability, and chlorine resistance, the proposed MMMs are examined using a dead-end reverse osmosis filtration setup. The results show that the active layer achieves an optimal permeation flux of 34.6 L/m 2 h, a natural sea salt rejection of 97%, and a chlorine resistance of 93%, suggesting that the proposed MMMs can be useful for seawater desalination.
Depravity of malaria in terms of morbidity and mortality in human beings makes it a major health ... more Depravity of malaria in terms of morbidity and mortality in human beings makes it a major health issue in tropical and subtropical areas of the globe. Drug counterfeiting and non-adherence to the treatment regimen have significantly contributed to development and spread of multidrug resistance that has highlighted the need for development of novel and more efficient antimalarial drugs. Complexity associated with cancer disease and prevalence of diversified cell populations vindicates highly specific treatment options for treatment of cancer. Resistance to these anticancer agents has posed a great hindrance in successful treatment of cancer. Pondering this ongoing situation, it was speculated to develop novel compounds targeting malaria and cancer. Moving on the same aisle, we synthesized pyrazole acrylic acid based oxadiazole and amide derivatives using multi-step reaction pathways (6a-x; 6a'-h'). Schizont maturation inhibition assay was employed to determine antimalarial po...
This work is concerned with the modelling of the interaction of fluid flow with flexibly supporte... more This work is concerned with the modelling of the interaction of fluid flow with flexibly supported rigid bodies. The fluid flow is modelled by Lattice-Boltzmann Method, coupled to a set of ordinary differential equations describing the dynamics of the solid body in terms its elastic and damping properties. The time discretization of the body dynamics is performed via the Time Discontinuous Galerkin Method. Several numerical examples are presented and highlight the robustness and efficiency of the proposed methodology, by means of comparisons with previously published results. The examples show that the present fluid-structure method is able to capture vortexinduced oscillations of flexibly-supported rigid body.
New hydrazone incorporated triazines were designed and synthesized using an appropriate synthetic... more New hydrazone incorporated triazines were designed and synthesized using an appropriate synthetic route with regard to essential pharmacophores, and evaluated for their anticonvulsant activity through maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole-induced seizure (scPTZ) screenings. Among the tested compounds, 4-[{2-(5-(3-chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6k (MES ED50 54.31, scPTZ ED50 92.01) and 4-[{2-(5-(4-chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6r (MES ED50 46.05, scPTZ ED50 83.90) emerged as the most active anticonvulsant agents having GABAergic effects. Compounds 6k and 6r also showed lesser CNS depressant effect than the standard drug carbamazepine. To obtain further insights into the binding interactions of these molecules, molecular docking studies were carried out.
Abstract: Several 3-chloro-4-flourophenyl substituted semicarbazones have been synthesized in thr... more Abstract: Several 3-chloro-4-flourophenyl substituted semicarbazones have been synthesized in three steps involving aryl urea and aryl semicarbazide formation. The structures have been confirmed by spectral and elemental analyses. Some selected ...
Abstract A new series of N-(6-chlorobenzothiazol-2-yl)-2-substituted-acetamides (3ah) and N-(6-c... more Abstract A new series of N-(6-chlorobenzothiazol-2-yl)-2-substituted-acetamides (3ah) and N-(6-chlorobenzothiazol-2-yl)-2-(substituted-benzylidene) hydrazinecarbothioamides (5ah) were synthesized and characterized by IR, 1 H NMR, mass and elemental analysis. In vivo ...
In order to produce new lead for an xio lytic and antidepressant drug, a new series of quinazolin... more In order to produce new lead for an xio lytic and antidepressant drug, a new series of quinazoline analogues was designed to mimic ATC-0175 structural features and fitted with functional groups believed to enhance an xio lytic and antidepressant activity. The synthesized co mpounds were evaluated for an xiolytic and antidepressant activity by elevated plus-maze and tail-suspension method. The targeted compounds (SKF 1-15) were synthesized fro m 2-chlo ro-6,7-dimetho xy quinazolin-4-amine and N-(substituted benzyl) propan-1-amines in isoamy l alcohol med iu m under reflu x for 24 h. A ll the targeted compounds are new chemical entit ies and obtained in satisfactory yields (Table 1). The structures of synthesized compounds are in good agreement with their corresponding spectral data.
A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synt... more A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synthetic route and characterized by spectral analysis (IR, 1H NMR, 13C NMR and Mass). The anticonvulsant activity of the synthesized compounds was determined using doses of 30, 100, and 300 mg kg-1 against maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Six compounds exhibited protection in both models and 2-(1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene)-N-p-tolylsemicarbazone emerged as the most active compound of the series without any neurotoxicity and significant CNS depressant effect. Liver enzyme estimations (SGOT, SGPT, Alkaline phosphatase) of the compound also showed no significant change in the enzymes levels. Moreover, it caused 80% elevation of γ-amino butyric acid (GABA) levels in the whole mice brain, thus indicating that it could be a promising candidate in designing of a potent anticonvulsant drug.
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