title: Design and synthesis of biquinolone-isoniazid hybrids as a new class of antitubercular and antimicrobial agents.
abstract: Twenty four biquinolone-isoniazid hybrids were designed based on molecular hybridization technique and synthesized via multicomponent cyclocondensation (MCC) approach. All the newly synthesized compounds were screened for their antimicrobial and antitubercular activities. The brine shrimp bioassay was carried out to study the cytotoxicity of the synthesized compounds. Hybrids 7f (MIC = 25 μg/mL); 7a, 7e and 7m (MIC = 50 μg/mL); 7g, 7h and 7k (MIC = 62.5 μg/mL) exhibited excellent antimicrobial activity as compared with standard drugs. Hybrids 7l and 7j displayed 99% inhibition against Mycobacterium tuberculosis bacteria with better LC50 values 35.39 and 34.59 μg/mL, respectively. These results indicate that the synthesized compounds can act as leads for the development of newer antimicrobial and antitubercular compounds.
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388120, Gujarat, India.
authors.forename: Hardik H
authors.initials: HH
authors.lastname: Jardosh
authors.forename: Manish P
authors.initials: MP
authors.lastname: Patel
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001156:Artemia; D001419:Bacteria / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005658:Fungi / Q000187:drug effects*; D007538:Isoniazid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000995:Antitubercular Agents; D015363:Quinolones; D007538:Isoniazid
keywords: Antimicrobial activity; Antitubercular activity; BDCPZPRQQFRLNL-UHFFFAOYSA-N; Biquinolone; Cytotoxicity; DSOHGANVGOSMPM-UHFFFAOYSA-N; FCYPZROBCDVQTL-UHFFFAOYSA-N; FEQRWCDJUSBYOQ-UHFFFAOYSA-N; HVXSEOAIUTYTMZ-UHFFFAOYSA-N; IFCWCIBEUQSYSN-UHFFFAOYSA-N; Isoniazid; JHRYNUYKSDABIU-UHFFFAOYSA-N; JOSWUCKHDVDNEP-UHFFFAOYSA-N; KHWMFBQIEQMQIK-UHFFFAOYSA-N; KKVNHMAOPLVKLF-UHFFFAOYSA-N; KPWZPEHNCYGXBV-UHFFFAOYSA-N; LPBILSMOKANMMT-UHFFFAOYSA-N; MHVCUGRMHUICGD-UHFFFAOYSA-N; MPENGEYHCDBKNT-UHFFFAOYSA-N; Multicomponent reaction; NASQFAHDWBWXBO-UHFFFAOYSA-N; NBLJSOPRECEKPC-UHFFFAOYSA-N; PFGZRXUPLKHNNS-UHFFFAOYSA-N; QGKRBTAAGBUEDC-UHFFFAOYSA-N; QZOKSQHTMCNROZ-UHFFFAOYSA-N; RAZHTFVRJYBRRE-UHFFFAOYSA-N; XAANNKSNOJAUTN-UHFFFAOYSA-N; XZWDOWJXEFEWJP-UHFFFAOYSA-N; YQSKWVJFMBTSQP-UHFFFAOYSA-N; YYGJYJDENSRLMU-UHFFFAOYSA-N