Identification of New Diamine Scaffolds with Activity Against Mycobacterium Tuberculosis.
From: Sequella, Inc., 9610 Medical Center Drive, Suite 200, Rockville, Maryland 20850, USA. elenabogatcheva@sequella.com
Journal of medicinal chemistry
- Publish Date: Jun 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 11
- Pages: 3045-8
- Medium: Print
- Language: English
- Citation (JAMA): Bogatcheva Elena, Hanrahan Colleen, Nikonenko Boris, et al. Identification of New Diamine Scaffolds with Activity Against Mycobacterium Tuberculosis.. J. Med. Chem. Jun 2006;49:3045-8
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.
Mesh Headings (Keywords): Animals, Antitubercular Agents, Biological Availability, Combinatorial Chemistry Techniques, Diamines, Mice, Mice, Inbred C3H, Microbial Sensitivity Tests, Mycobacterium tuberculosis, Piperazines, Piperidines, Structure-Activity Relationship, Tuberculosis, Pulmonary
Check for Full Text / PubMed Unique Identifier (PMID): 16722620
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