Discovery of New Antitubercular Oxazolyl Thiosemicarbazones

Twenty 4-(5-cyclobutyloxazol-2-yl)thiosemicarbazones were synthesized and evaluated for preliminary in vitro and in vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Among them, (4-bromophenyl)(phenyl)methanone N-(5-cyclobutyl-1...

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Published in:Journal of medicinal chemistry 2006-06, Vol.49 (12), p.3448-3450
Main Authors: Sriram, Dharmarajan, Yogeeswari, Perumal, Thirumurugan, Rathinasababathy, Pavana, Roheet Kumar
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics, Antitubercular - chemical synthesis
Antibiotics, Antitubercular - chemistry
Antibiotics, Antitubercular - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Drug Resistance, Multiple, Bacterial
Medical sciences
Microbial Sensitivity Tests
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Structure-Activity Relationship
Thiosemicarbazones - chemical synthesis
Thiosemicarbazones - chemistry
Thiosemicarbazones - pharmacology
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Summary:Twenty 4-(5-cyclobutyloxazol-2-yl)thiosemicarbazones were synthesized and evaluated for preliminary in vitro and in vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Among them, (4-bromophenyl)(phenyl)methanone N-(5-cyclobutyl-1,3-oxazol-2-yl)thiosemicarbazone 6q was found to be the most active compound in vitro with minimum inhibitory concentration of 0.05 μg/mL against MTB and MDR-TB. In the in vivo animal model 6q decreased the bacterial load in lung and spleen tissues with 2.1 log 10 and 3.72 log 10 protections, respectively, at 50 mg/kg body weight dose.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm060339h