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环己基格雷西霉素对小鼠中的脓肿分枝杆菌具有活性。

Cyclohexyl-griselimycin Is Active against Mycobacterium abscessus in Mice.

机构信息

Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.

Evotec ID (Lyon) SAS, Lyon, France.

出版信息

Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0140021. doi: 10.1128/AAC.01400-21. Epub 2021 Nov 1.

DOI:10.1128/AAC.01400-21
PMID:34723632
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8765428/
Abstract

Cyclohexyl-griselimycin is a preclinical candidate for use against tuberculosis (TB). Here, we show that this oral cyclodepsipeptide is also active against the intrinsically drug-resistant nontuberculous mycobacterium Mycobacterium abscessus and in a mouse model of infection. This adds a novel advanced lead compound to the M. abscessus drug pipeline and supports a strategy of screening chemical matter generated in TB drug discovery efforts to fast-track the discovery of novel antibiotics against M. abscessus.

摘要

环己基格雷西霉素是一种用于治疗结核病（TB）的临床前候选药物。在这里，我们表明，这种口服环二肽也对固有耐药的非结核分枝杆菌脓肿分枝杆菌有效，并在感染的小鼠模型中也有效。这为脓肿分枝杆菌药物研发管道添加了一种新型先导化合物，并支持了一种筛选结核药物发现工作中产生的化学物质的策略，以加快发现针对脓肿分枝杆菌的新型抗生素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/6dd51cf9558b/aac.01400-21-f003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/67e87c44940a/aac.01400-21-f001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/4bdc67f2c999/aac.01400-21-f002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/6dd51cf9558b/aac.01400-21-f003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/67e87c44940a/aac.01400-21-f001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/4bdc67f2c999/aac.01400-21-f002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2146/8765428/6dd51cf9558b/aac.01400-21-f003.jpg

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