10.1016/j.bmcl.2016.06.038
The study focuses on the synthesis, identification, and in vitro biological evaluation of novel quinoline-incorporated 1,3-thiazinan-4-one derivatives. Two new series of compounds, 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a-j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one derivatives (5a-7j), were synthesized through a one-pot three-component cyclo-condensation reaction. These compounds were characterized using FT-IR, 1H, 13C NMR, and elemental analysis. Their in vitro biological activities were assessed for antibacterial effects against various pathogenic bacterial strains, antitubercular activity against Mycobacterium Tuberculosis H37Rv, and antimalarial activity against Plasmodium falciparum. The study identified certain compounds, particularly 4f and 5f, that exhibited excellent antibacterial and antitubercular activities, along with good antimalarial activity, comparing favorably with frontline drugs. The findings suggest potential for these compounds as new antimicrobial, antitubercular, and antimalarial agents.
10.1016/j.ejmech.2011.01.066
The research focuses on the synthesis and anticancer activities of novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones, which are compounds designed to target and inhibit the proliferation of cancer cells. The purpose of this study was to evaluate the in vitro antiproliferative activities of these compounds against four human cancer cell lines: MDA-MB-435 (breast), HL-60 (leukemia), HCT-8 (colon), and SF-295 (central nervous system). The synthesis involved the use of reagents like diethylethoxymethylenemalonate, thionyl chloride, and 2-hydrazinobenzothiazole, among others, to construct the target molecules.
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