title: Antimycobacterial activity of diospyrin derivatives and a structural analogue of diospyrin against Mycobacterium tuberculosis in vitro.
abstract: Three derivatives and one structural analogue of diospyrin were synthesized and investigated for their inhibitory activity against Mycobacterium tuberculosis employing the rapid radiometric method in vitro. A novel aminoacetate derivative was found to be more active than the parent compound, the MICs being 50 and 100 mg/L, respectively, for a drug-susceptible strain, H37Rv, of M. tuberculosis. This derivative also exhibited an MIC of 50 mg/L for a few multidrug-resistant strains of M. tuberculosis. The other two derivatives and the analogue did not show any significant antimycobacterial activity at the highest concentration (100 mg/L) tested.
authors.affiliation: Department of Botany, University of Pretoria, Pretoria 0002, South Africa.
authors.forename: N
authors.initials: N
authors.lastname: Lall
authors.forename: M
authors.initials: M
authors.lastname: Das Sarma
authors.forename: B
authors.initials: B
authors.lastname: Hazra
authors.forename: J J M
authors.initials: JJ
authors.lastname: Meyer
mesh_terms: D000904:Antibiotics, Antitubercular / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D004977:Ethambutol / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000378:metabolism; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D010101:Oxygen Consumption / Q000187:drug effects; D024301:Plant Bark / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry; D013307:Streptomycin / Q000494:pharmacology
chemical_list: D000904:Antibiotics, Antitubercular; D000995:Antitubercular Agents; D009285:Naphthoquinones; D004977:Ethambutol; C043546:diospyrin; D013307:Streptomycin