Thiazolidinones are heterocyclic organic medicines and the antifungal, antibacterial, and antiproliferative effects were shown in the studies. The aim of the study was to investigate the possible negative effects of (4S)-2-(4-hydroxy-3-methoxyphenyl)thiazolidine-4-carboxylic acid in zebrafish testicular tissue on an ultrastructural level. Experimental groups were exposed to different doses (0.2mM, 0.4mM, and 0.6mM) of thiazolidinone for 5 days. Further, no treatment was given to the control group. The testicular tissues were fixed and embedded in epoxy resin. The pathological sections were evaluated with transmission electron microscope. The sertoli, leydig, and spermatogenic cells of the control group showed intact morphology. In experimental groups, mitochondrial swelling, intense cristae loss, and autophagic vacuoles were observed in the Sertoli cells. Dilated perinuclear space, mitochondrial degeneration, and dilated smooth endoplasmic reticulum (sER) were detected in spermatocytes. The spermatids showed separation between genetic material and nuclear membrane. The condensation of genetic material was irregular. Mitochondrial degeneration and dilatation of sER tubules were detected. The Leydig cells showed perinuclear space dilatation, mitochondria degeneration, and dilatation in sER tubules. Our findings suggest that thiazolidinone has degenerative effects on zebrafish testis and this chemical should be carefully used in the pharmaceutical industry.
چکیده:
In this research article, we report the preparation of from melamine-terephthalaldehyde supported Copper-1,2,4,5-tetrabenzenecarboxylic acid (COF-MOF) as a porous acidic catalyst for the one-pot preparation of 1,8-Dioxooctahydroxanthenes. As a new methodology, this strategy offers several advantages including green reaction conditions, high yield of the products, short reaction time, facile work-up, and recyclability of the catalyst.
Present study investigated the effect of tobacco-specific carcinogen, nicotine-derived nitrosamine ketone (NNK), on the expression of cellular stress response genes in lung tissue of Wistar rats. Moreover, the effect of exercise training on alterations of these genes in exposed rats was investigated.
Materials and Methods
A total of 30 healthy Wistar rats were obtained and divided into the following group: (1) Control (CON), (2) NNK exposure (NNK, once a week / 12.5 mg per kg body mass for 12 weeks), and NNK + swimming training (NNK+ST, received NNK exposure + 25-60 min of aerobic swimming training / 5 days per week for 12 weeks). The mRNA expression level of nuclear factor kappa-B (NF-κB), forkhead box protein O3 (FOXO3), and Sirtuin-1 (Sirt-1) were determined in lung tissue by the quantitative real-time PCR.
Results
The NNK exposure resulted in a significant reduction in mRNA expression of the NF-κB and FOXO3 (P=0.0001 and P=0.005, respectively), as well as a significant increment in mRNA expression of Sirt-1 (P=0.001) comparing to the CON group. Moreover, the ST in rats under NNK treatment led to a significant reduction in mRNA expression of NF-κB (P=0.0001), but it did not have any significant effect on mRNA expression of FOXO3 and Sirt-1 (P>0.05) comparing to the NNK group.
Conclusion
These findings indicate that NNK exposure can lead to adverse alterations in the expression of cellular stress response genes in the lung tissue of Wistar rats and exercise training may not have any favorable effect on the expression of these genes in rats under NNK treatment.
چکیده:
In this study, N-(2,4,6-tribromophenyl)maleimide (TBPMI) was synthesized using three different catalysts, including stannous chloride, anhydrous acetic acid, and phosphoric acid, respectively. Comparative analysis was carried out on the synthesis conditions and the yields of TBPMI synthesized using different catalysts. Infrared spectroscopy and nuclear magnetic resonance spectroscopy were employed to characterize TBPMI. Results showed that the use of phosphoric acid as the catalyst required harsh reaction conditions and also the catalytic efficiency was poor. On the other hand, under similar conditions, the catalytic efficiency of anhydrous acetic acid was higher than that of stannous chloride, along with the reduction in problems associated with erosion and pollution.
Viral outbreaks are a common cause of morbidity and mortality in livestock and human populations. Lack of good vaccines and poor control measures along with natural viral genetic drifting and shifting are the common causes of new viral strains and outbreaks. The current study reports the synthesis of some 2-aryl substituted thiazolidine-4-carboxylic acids 1a-h and their 3-acetyl 2a and 3-benzoyl derivatives 3a. Two important poultry viruses: Avian influenza virus (AIV; A/Chicken/Italy/1994/H9N2) and infectious bronchitis virus (IBV) were selected, grown in 9-11 days old chicken embryonated eggs, and subjected to in ovo anti-viral assays. Most of the synthesized compounds were found active against AIV subtype H9N2 and IBV. In the case of AIV, the best results were attained for compound 1d which showed an IC50 value of 3.47 µM, while IBV 1c showed IC50 valueof4.10 µM. The lower IC50 values of these compounds correlate with the high potency of these compounds, especially in comparison with control groups. The standard drugs amantadine and ribavarin were used as positive controls in the case of AIV and IBV, respectively. Better results were obtained with 2-aryl substituted thiazolidine-4-carboxylic acids 1a-h compared to their N-acylated derivatives 2a and 3a against both viruses. In conclusion, this preliminary data support the idea that thiazolidine carboxylic acids could be used as anti-viral drugs against AIV and IBV infections.
چکیده:
We report here an efficient and green method for fused Biginelli condensation reaction of aldehydes, cyclopentanone, and urea catalyzed by nano ZrO2-SO3H under solvent-free conditions. The prospect of the reusability of this catalyst has also been demonstrated without compromising on the yield of the product. On the whole, the protocol presented here is an excellent alternative to many of the previously reported procedures. So, Optimized molecular structures have been investigated by DFT/B3LYP method with 6-31G (d,p) basis set. Stability of some 4-aryl-7-benzylidene-1,3,4,5,6,7-hexahydro-4-phenyl-2H-cyclopenta[d]pyrimidin-2-one (2 a-j) derivatives and intramolecular interactions bond has been analyzed by using natural bond orbital (NBO) analysis.
The aim of the present study is to investigate the in vitro and in vivo antidiabetic activity of 4-amino-5-benzofuran-2-oyl-2-(4-methoxyphenyl)aminothiazole. Toxicity and in vitro antidiabetic study of the compound was carried out in L6 cell lines. In vivo antidiabetic studies were carried out in alloxan induced diabetic Wistar albino rats. In toxicity study, the compound showed an IC50 value of 973.62 µM. Significant changes in glucose uptake and Glut 4 translocation by 4-amino-5-benzofuran-2-oyl-2-(4-methoxyphenyl)aminothiazole suggested that the molecular mechanism of action is similar to that of insulin. In vivo treatment with 4-amino-5-benzofuran-2-oyl-2-(4-methoxyphenyl)aminothiazole at a concentration of 60 mg/kg bodyweight significantly decreased blood glucose and glycosylated haemoglobin levels in diabetic rats than in non-diabetic control rats. Oral administration of 4-amino-5-benzofuran-2-oyl-2-(4-methoxyphenyl)aminothiazole to the experimental groups also showed a highly significant reduction in total cholesterol level when compared with diabetic control rats These findings revealed that 4-amino-5-benzofuran-2-oyl-2-(4-methoxyphenyl)aminothiazole can be considered as a lead molecule for the control of type II diabetes.
New 1,5-tetra alkyl methyl- phenyl-1H-pyrimido[4,5-e][1,3,4]thiadiazine-3,7-diamine were synthesized via the cyclocondensation of 2-(5-bromo-2-chloro-6-methylpyrimidin-4-yl)-2- methylhydrazine with phenylthioisothiocyanate and further replacement of chlorine atom on the seven number position of pyrimido[4, 5- e][1, 3, 4]thiadiazin by appropriate secondary amines in simple and efficient methods.
چکیده:
A simple, sensitive, and non-extractive spectrophotometric method was developed for the determination of copper (II) using a newly synthesized chromogenic reagent, 6-(phenanthrene-3-yl)-1,2,4,-triazine-3-thione(PhDTT), in Tween 80 neutral surfactant. To synthesize the reagent (PhDDT), amyl nitrite was added to 3-acethylphenanthrene and refluxed for 26 hours to produce 2-oxo-2-(phenanthren-3-yl) acetaldehyde oxime (I). The reaction of compound (I) with thiosemicarbazide yielded the reagent (PhDDT). Copper (II) forms a red colored complex with 6-(phenanthrene-3-yl)-1,2,4,-triazine-3-tion which shows maximum absorbance at 460 nm in the pH range 9.0-11.0. Beer’s law was obeyed over the concentration range of 1.4-10 µg/mL Cu2+ with r2 = 0.999. The limit of detection was 0.48 μg/mL of copper (II). The within-day and between-day precision values were in the range of 0.38-3.3%. The method was tested by analyzing the amalgam samples. The results were in good agreement with the atomic absorption.
چکیده:
An efficient and convenient method for synthesis of 2,6-bis (4-(dialkylamino) styryl)-4H-pyran-4-one starting from 4- (dialkylamino) benzaldehyde with 2,6-dimethyl-4H-pyran-4-onein the presence of MeONa as the base was described. Additionally, preparation of novel compounds with bis-DCM-type skeleton for application in organic light-emitting diodes was developed via reaction of malononitrile as active methylene group with 2,6-bis (4-(dialkylamino) styryl) -4H-pyran-4-one derivatives. 1H and 13C NMR, FT-IR spectroscopy supported the predicted structure of the products. The UV-Vis absorption spectra of synthesis compound were measured in diluted dichloromethane solution. Maximum absorption (lmax) values differ from 460 to 496 nm, this absorption is due to π-π* transition.
