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MicrobiologybioRxiv

Mycobacterium tuberculosis DprE1 inhibitor OPC-167832 is active against Mycobacterium abscessus in vitro

J. P. Sarathy, M. Zimmerman, M. Gengenbacher, V. A. Dartois, T. Dick

Abstract

The anti-tuberculosis candidate OPC-167832, an inhibitor of DprE1, was active against Mycobacterium abscessus. Resistance mapped to M. abscessus dprE1, suggesting target retention. OPC-167832 was bactericidal and did not antagonize activity of clinical anti-M. abscessus antibiotics. Due to its moderate potency compared to Mycobacterium tuberculosis, the compound lacked efficacy in a mouse model and is thus not a repurposing candidate. These results identify OPC-167832 - DprE1 as a lead-target couple for a M. abscessus-specific optimization program.

PDFDOI

02 /Specification & Classification

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