title: Novel 1-(4-substituted benzylidene)-4-(1-(substituted methyl)-2,3-dioxoindolin-5-yl)semicarbazide derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) and MDR-TB strain.
abstract: A series of eighteen new 1-(4-substituted benzylidene)-4-(1-(substituted methyl)-2,3-dioxoindolin-5-yl)semicarbazide derivatives were designed, synthesized and characterized by spectral and elemental analyses. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) and MDR-TB strains. The activity was expressed as the minimum inhibitory concentration in μg/mL. Among the tested compounds 7j, 7m, 7o and 7q possesses equipotent activity as standard drug Isoniazid against MTB while 7m and 7q exhibited higher activity against MDR-TB strain when compared with both the reference drugs isoniazid and rifampicin. Basic structure activity relationships are presented.
authors: Department of Pharmaceutical Chemistry, GITAM Institute of Pharmacy, GITAM University, Visakhapatnam, Andhra Pradesh, India.
authors: Sundararajan
authors: S
authors: Raja
authors: Chinnasamy Rajaram
authors: CR
authors: Prakash
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D012663:Semicarbazides / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy* / Q000382:microbiology
chemical_list: D000995:Antitubercular Agents; D012663:Semicarbazides