Two series of 3-substituted-7-methyl-5,6,7,8-tetrahydropyrido[4',3':4,5] thieno[2,3-d]pyrimidin-4(3H)-one (6a-k) and 3-substituted-7,2-dimethyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one (7a-k) derivatives were synthesized and characterized using spectral data i.e., IR, 1H-, 13C-NMR, Mass and CHN elemental analyses. The synthesized compounds were evaluated for antibacterial activity against each of two strains of Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Klebsiella pneumoniae) bacteria and antimycobacterial activity screened against two strains i.e., Mycobacterium tuberculosis (MTB) H37Rv and an isoniazid-resistant clinical sample. Further to validate potentiality of our design was analyzed using molecular docking studies by taking crystal structure of MTB pantothenate synthetase (MTB-PS) (PDB: 3IVX). In this study, some compounds 6k (Minimum Inhibitory Concentration (MIC): MIC-22 µM), 7d (MTB: MIC-22 µM) and 7k (MTB: MIC-11 µM) showed potential antibacterial and antimycobacterial activities.
In the present work, the preliminary phytochemical study and in vitro thrombolytic activity was conducted for Terminalia pallida Brandis leaves extract. In vitro thrombolytic was evaluated by clot lysis effect of different solvent extracts of Terminalia pallida Brandis leaves. In this study, streptokinase and distilled water were used as positive control and negative control, respectively. In vitro thrombolytic model of methanolic extract showed maximum clot lysis (95.43%±0.697) at test concentration (800μg/ml) in 72 hrs. Hydro alcoholic extract also showed potential clot lysis (90.43%±0.748) at similar test conditions. In addition, other plant extracts such as petroleum ether, ethyl acetate, chloroform extract showed moderate activity at 800 μg/ml concentration i.e., 65.56%±0.984, 70.16%±0.325 and 72.98%±0.985 clot lysis, respectively in 72 hrs. Streptokinase (SK) and water showed clot lysis maximum of 97.26%±0.974 and 41.33%±0.843 respectively. The present study reveals that the methanolic and hydro alcoholic extracts of Terminalia pallida Brandis leaves possesses potential thrombolytic activity.