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

doi:10.1021/jm050948+

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 journal › Article › peer-review

96 Scopus citations

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 language	English (US)
Pages (from-to)	3045-3048
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	49
Issue number	11
DOIs	https://doi.org/10.1021/jm050948+
State	Published - Jun 1 2006
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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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.",

author = "Elena Bogatcheva and Colleen Hanrahan and Boris Nikonenko and Rowena Samala and Ping Chen and Jacqueline Gearhart and Francis Barbosa and Leo Einck and Nacy, {Carol A.} and Marina Protopopova",

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T1 - Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis

AU - Bogatcheva, Elena

AU - Hanrahan, Colleen

AU - Nikonenko, Boris

AU - Samala, Rowena

AU - Chen, Ping

AU - Gearhart, Jacqueline

AU - Barbosa, Francis

AU - Einck, Leo

AU - Nacy, Carol A.

AU - Protopopova, Marina

PY - 2006/6/1

Y1 - 2006/6/1

N2 - 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.

AB - 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.

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Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis

Abstract

ASJC Scopus subject areas

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