A series of 3-aryl indazoles and 1-methyl-3-aryl indazole derivatives are prepared with exceptional yields by coupling with several arylboronic acids and methylation by two dissimilar approaches. The as-prepared indazole derivatives (3a–3j) and their N-methyl derivatives (5a–5j) are evaluated for in vitro anticancer activity against two cancer cell lines, HCT-116 and MDA-MB-231. The results reveal that the indazole derivatives tested display mild to moderate anticancer activities against the cell lines tested.
Abstract. A series of 10 new hispolonpyrazole sulfonamides were designed and synthesized using hispolons and 4-sulfonamide phenylhydrazine hydrochloride with better yields. The synthesized pyrazole sulfonamides were screened for anti-TB, anti-bacterial, and anti-fungal activities to compare the role sulfonamide moiety. Among them, 3a and 3b showed selective potent anti-tubercular nature (MIC 6.25µg/mL). Further, the antimicrobial studies of the compounds showed only compound 3b with a good inhibition zone on Staphylococcus aureus among other bacteria and fungi studied.
Resumen.Se prepararon 10 nuevas hispolon-pirazol-suklfonamidas con buenos rendimientos haciendo reaccionar hipolonas y el clorhidrato de 4-sulfonamidil-fenílhidrazina. Los productos obtenidos se probaron contra cepas de hongos y bacterias con especial interés en la tuberculosis, encontrando algunos derivados con actividades del orden de MIC 6.25µg/mL.
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