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Fourteen novel dipeptide carboxamide derivatives bearing benzensulphonamoyl propanamide were synthesized and characterized using 1 H NMR, 13 C NMR, FTIR and MS spectroscopic techniques. In vivo antimalarial and in vitro antimicrobial studies were carried out on these synthesized compounds. Molecular docking, haematological analysis, liver and kidney function tests were also evaluated to assess the effect of the compounds on the organs. At 200 mg/kg body weight, 7i inhibited the multiplication of the parasite by 81.38% on day 12 of post-treatment exposure. This was comparable to the 82.34% reduction with artemisinin. The minimum inhibitory concentration (MIC) in µM ranged from 0.03 to 2.34 with 7h having MIC of 0.03 µM against Plasmodium falciparium. The in vitro antibacterial activity of the compounds against some clinically isolated bacteria strains showed varied activities with some of the new compounds showing better activities against the bacteria and the fungi more than the reference drug ciprofloxacin and fluconazole.

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We have designed and synthesized novel 7-substituted-3acetyl-benzopyrones 9 a-9 g and ethyl 7-substituted-3-carboxylate-benzopyrones 10 a-10 d and screened for anticancer activity using MTT assay. Most of the tested compounds have shown very good activity against A549 cell line (lung cancer cell-line) and MCF7 cell line (breast cancer cell-line) compared to 5-Fluorouracil. Compound 9 b and 9 e exhibited excellent anticancer activity with IC 50 0.16 nM against A549 cell line and 84.8 nM against MCF7 cell line respectively. Compounds 9 b and 9 e showed excellent anticancer activity at very low concentration, well falling in nanomolar region. Compounds 9 b and 9 e exhibited very good binding constant for DNA binding through intercalation in UV based DNA titration which was further confirmed by fluorescence based EtBr displacement assay in DNA-EtBr complex.[a] S.