Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis

Elena Bogatcheva, Colleen Hanrahan, Boris Nikonenko, Rowena Samala, Ping Chen, Jacqueline Gearhart, Francis Barbosa, Leo Einck, Carol A. Nacy, Marina Protopopova

Research output: Contribution to journalArticlepeer-review

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 μM. New prospective scaffolds with antitubercular activity derived from homopiperazine, 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.

Original languageEnglish (US)
Pages (from-to)3045-3048
Number of pages4
JournalJournal of medicinal chemistry
Volume49
Issue number11
DOIs
StatePublished - Jun 1 2006
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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