A novel series of hydrazonothiazolidinyl acetic acid derivatives were synthesized via a straightforward microwave irradiated one‐pot multicomponent reaction approach using substituted 3‐acetylcoumarins (1a‐l), thiosemicarbazide (2), and maleic anhydride (3). The synthesis was carried out by using sodium acetate and acetic acid as a solvent at 70°C, afforded target molecules in a shorter reaction time, simple reaction workup with high yields. All the synthesized compounds were well characterized by analytical data (1H, 13C NMR and mass spectra). In vitro antiviral activity of thiazolidinyl acetic acid derivatives were evaluated against a broad panel of human viruses in different cell lines among which compound 4d exhibited excellent activity against Herpes simplex virus‐1.
A novel series of dihydropyrazolyl bithiazoles were efficiently synthesized through simple reaction conditions via one pot multicomponent reaction of 2-bromo-1-(4-methyl-2-phenyl thiazol-5-yl)ethan-1-one (1), thiosemicarbazide (2) and chalcones (3 a-k) in the presence of sodium hydroxide in ethanol under reflux condition. The reaction generates two potential five membered heterocylic pharmacophores i.e. Hantzsch thiazole and dihydropyrazole in one step through operational simplicity, shorter reaction time with high yields. The newly synthesized compounds were well characterized by IR, 1H, 13C NMR and Mass spectral data. All the newly synthesized compounds were evaluated for their anticancer activity against human cancer cell lines and calculated their binding energy values with respect to 3ert protein. The compounds 4f, 4g, 4h and 4j exhibited excellent activity against MCF-7 cancer cell line with IC50 Values of 3.47 ± 0.28, 1.36 ± 0.74, 3.76 ± 0.35 and 4.14 ± 0.26 µM concentrations and studied molecular interaction of probable target protein human Estrogen Receptor Alpha protein (3ert.pdb) using docking simulation.
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