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Oxadiazoles Have Butyrate-Specific Conditional Activity against Mycobacterium tuberculosis.

ABSTRACT: Mycobacterium tuberculosis is a global pathogen of huge importance which can adapt to several host niche environments in which carbon source availability is likely to vary. We developed and ran a phenotypic screen using butyrate as the sole carbon source to be more reflective of the host lung environment. We screened a library of ?87,000 small compounds and identified compounds which demonstrated good antitubercular activity against M. tuberculosis grown with butyrate but not with glucose as the carbon source. Among the hits, we identified an oxadiazole series (six compounds) which had specific activity against M. tuberculosis but which lacked cytotoxicity against mammalian cells.

SUBMITTER: Early JV

PROVIDER: S-EPMC4879361 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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Oxadiazoles Have Butyrate-Specific Conditional Activity against Mycobacterium tuberculosis.

Early Julie V JV Casey Allen A Martinez-Grau Maria Angeles MA Gonzalez Valcarcel Isabel C IC Vieth Michal M Ollinger Juliane J Bailey Mai Ann MA Alling Torey T Files Megan M Ovechkina Yulia Y Parish Tanya T

Antimicrobial agents and chemotherapy 20160523 6

Mycobacterium tuberculosis is a global pathogen of huge importance which can adapt to several host niche environments in which carbon source availability is likely to vary. We developed and ran a phenotypic screen using butyrate as the sole carbon source to be more reflective of the host lung environment. We screened a library of ∼87,000 small compounds and identified compounds which demonstrated good antitubercular activity against M. tuberculosis grown with butyrate but not with glucose as the ...[more]

PMID: 27044545

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