Activity of Tricyclic Pyrrolopyrimidine Gyrase B Inhibitor against Mycobacterium abscessus

Autor:	Abdeldjalil Madani, Dereje A. Negatu, Abdellatif El Marrouni, Randy R. Miller, Christopher Boyce, Nicholas Murgolo, Christopher J. Bungard, Matthew D. Zimmerman, Véronique Dartois, Martin Gengenbacher, David B. Olsen, Thomas Dick
Rok vydání:	2022
Předmět:	Adenosine Triphosphatases Pharmacology Mycobacterium abscessus Mycobacterium Infections Nontuberculous Nontuberculous Mycobacteria Microbial Sensitivity Tests Anti-Bacterial Agents Mice Pyrimidines Infectious Diseases DNA Gyrase Animals Pyrroles Pharmacology (medical)
Zdroj:	Antimicrobial Agents and Chemotherapy. 66
ISSN:	1098-6596 0066-4804
Popis:	Tricyclic pyrrolopyrimidines (TPPs) are a new class of antibacterials inhibiting the ATPase of DNA gyrase. TPP8, a representative of this class, is active against Mycobacterium abscessus in vitro. Spontaneous TPP8 resistance mutations mapped to the ATPase domain of M. abscessus DNA gyrase and the compound inhibited DNA supercoiling activity of recombinant M. abscessus enzyme. Further profiling of TPP8 in macrophage and mouse infection studies demonstrated proof-of-concept activity against M. abscessus ex vivo and in vivo.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37177682f6362f871ef2526a318de268 https://doi.org/10.1128/aac.00669-22 Zobrazit plný text záznamu