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A series of 2-methylthio-1,4-dihydropyrimidine derivatives (IIa-IIl) were synthesized in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (Ia-Il) with methyl iodide in the presence of pyridine. Their structures were confirmed by elemental analysis, IR, and 1H NMR spectra. Molecular docking of title compounds was done using VLife MDS 3.5 on voltage-dependent calcium channel b subunit functional core and its complex with the a1 interaction domain i.e. AID-b complex (PDB code 1T3L) to identify potential candidates with minimum dock score for cardioprotective activity. Biological screening of the potential candidates (IIf and IIi) was done for cardioprotective activity. Adult Sprague-dawley rats were pretreated with test compounds IIf and IIi. After the treatment period, adrenaline was subcutaneously injected to rats at an interval of 24 h for 2 days to induce myocardial injury. After 48 h, rats were anaesthetized and electrocardiographic (ECG) observations were performed. Potential compounds IIf and IIi showed significant cardioprotective activity against adrenaline-induced myocardial infarction in rats. Adrenaline-induced ECG alterations such as reduced R-R interval, increased heart rate, reduced P duration, and ST-segment elevation were brought to the near normal values by pretreatment of compounds IIf and IIi.

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Present work describes the potent antidiabetic fraction from flowers of Cassia auriculata Linn. Hydromethanolic extract along with its ethyl acetate and n-butanol fractions were evaluated for antidiabetic activity in alloxan-induced diabetes in rats. The n-butanol fraction exhibited significant reduction (p<0.001) in blood glucose levels and was also found effective in restoring the blood lipids and proteins to normal level. The activity was found comparable with standard drug phenformin. The hydromethanolic extract and its fractions were subjected to preliminary qualitative chemical investigations which indicated the presence of phenolic compounds, carbohydrates, tannins, steroids and amino acids.

In continuation with our research program, in search of potent enzyme tyrosinase inhibitor, a series of synthesized 2,5-disubstituted 1,3,4-oxadiazoles have been evaluated for enzyme tyrosinase inhibitory activity. Subsequently, 3D QSAR and docking studies were performed to find optimum structural requirements for potent enzyme tyrosinase inhibitor from this series. The synthesized 20 compounds of 2,5-disubstituted-1,3,4-oxadiazole series were screened for mushroom tyrosinase inhibitory activity at various concentrations by enzyme inhibition assay. The percentage enzyme inhibition was calculated by recording absorbance at 492 nm with microplate reader. 3D QSAR and docking studies were performed using VLife MDS 3.5 software. In the series 2,5-disubstituted-1,3,4-oxadiazoles enzyme tyrosinase inhibitory activity was found to be dose dependent with maximum activity for compounds4c,4h,4m, and4r. 3D QSAR and docking studies revealed that more electropositive and less bulky substituents if placed on 1,3,4-oxadiazole nucleus may result in better tyrosinase inhibitory activity in the series.