biostudies-literatureUnknown13(1)Pham ECCompounds containing benzimidazole moiety occupy privileged chemical space for discovering new bioactive substances. In continuation of our recent work, 69 benzimidazole derivatives were designed and synthesized with good to excellent yields of 46-99% using efficient synthesis protocol <i>i.e.</i> sodium metabisulfite catalyzed condensation of aromatic aldehydes with <i>o</i>-phenylenediamines to form 2-arylbenzimidazole derivatives followed by <i>N</i>-alkylation by conventional heating or microwave irradiation for diversification. Potent antibacterial compounds against MSSA and MRSA were discovered such as benzimidazole compounds 3k (2-(4-nitrophenyl), <i>N</i>-benzyl), 3l (2-(4-chlorophenyl), <i>N</i>-(4-chlorobenzyl)), 4c (2-(4-chlorophenyl), 6-methyl, <i>N</i>-benzyl), 4g (2-(4-nitropRSC advances399-420https://www.ebi.ac.uk/biostudies/studies/S-EPMC9782508biostudies-literature<i>N</i>,2,6-Trisubstituted 1<i>H</i>-benzimidazole derivatives as a new scaffold of antimicrobial and anticancer agents: design, synthesis, <i>in vitro</i> evaluation, and <i>in silico</i> studies.PMC9782508Vu TTTruong TNTran Nguyen NVVo Thi BNBao Le KNPham ECVo DDLe Thi TVVong LBLy Hong HHfalse<i>N</i>,2,6-Trisubstituted 1<i>H</i>-benzimidazole derivatives as a new scaffold of antimicrobial and anticancer agents: design, synthesis, <i>in vitro</i> evaluation, and <i>in silico</i> studies.Compounds containing benzimidazole moiety occupy privileged chemical space for discovering new bioactive substances. In continuation of our recent work, 69 benzimidazole derivatives were designed and synthesized with good to excellent yields of 46-99% using efficient synthesis protocol <i>i.e.</i> sodium metabisulfite catalyzed condensation of aromatic aldehydes with <i>o</i>-phenylenediamines to form 2-arylbenzimidazole derivatives followed by <i>N</i>-alkylation by conventional heating or microwave irradiation for diversification. Potent antibacterial compounds against MSSA and MRSA were discovered such as benzimidazole compounds 3k (2-(4-nitrophenyl), <i>N</i>-benzyl), 3l (2-(4-chlorophenyl), <i>N</i>-(4-chlorobenzyl)), 4c (2-(4-chlorophenyl), 6-methyl, <i>N</i>-benzyl), 4g (2-(4-nitrop2022-01-01T00:00:00Z2022 Dec2026-05-27T21:04:30.068Z2025-04-04T08:34:49.698ZS-EPMC97825083660563010.1039/d2ra06667j