Antimycobacterial activity of diospyrin derivatives and a structural analogue of diospyrin against Mycobacterium tuberculosis in vitro.
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.
Lall
N
N
Department of Botany, University of Pretoria, Pretoria 0002, South Africa.
Das Sarma
M
M
Hazra
B
B
Meyer
J J M
JJ
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
D000904:Antibiotics, Antitubercular; D000995:Antitubercular Agents; D009285:Naphthoquinones; D004977:Ethambutol; C043546:diospyrin; D013307:Streptomycin