Identification of New Diamine Scaffolds with Activity against Mycobacterium tuberculosis
Journal of Medicinal Chemistry2006Vol. 49(11), pp. 3045–3048
Citations Over TimeTop 10% of 2006 papers
Elena Bogatcheva, Colleen F. Hanrahan, B. V. Nikonenko, Rowena Samala, Ping Chen, Jacqueline Gearhart, Francis Barbosa, Leo Einck, Carol A. Nacy, Marina Protopopova
Abstract
A diverse 5000-compound library was synthesized from commercially available diamines and screened for activity against Mycobacterium tuberculosis in vitro, revealing 143 hits with minimum inhibitory concentration (MIC) equal to or less than 12.5 microM. New prospective scaffolds with antitubercular activity derived from homo-piperazine, phenyl- and benzyl-substituted piperazines, 4-aminomethylpiperidine, 4-aminophenylethylamine, and 4,4'-methylenebiscyclohexylamine were identified. Compound SQ775 derived from homopiperazine and compound SQ786 derived from benzylpiperazine had potent antimicrobial activity against M. tuberculosis in experimental animals in vivo.
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