探索 4-氨基喹唑啉类化合物作为结核分枝杆菌 N-乙酰氨基葡萄糖-1-磷酸尿苷酰转移酶（GlmU）抑制剂的耐多药结核抑制潜力。
Exploring MDR-TB Inhibitory Potential of 4-Aminoquinazolines as Mycobacterium tuberculosis N-Acetylglucosamine-1-Phosphate Uridyltransferase (GlmU ) Inhibitors.
机构信息
Department of Pharmaceutical Chemistry, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban, 4000, South Africa.
Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, 425405, India.
出版信息
Chem Biodivers. 2020 Aug;17(8):e2000237. doi: 10.1002/cbdv.202000237. Epub 2020 Jul 20.
Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new antitubercular agents which operate via novel modes of action. Here, we are reporting on 4-aminoquinazolines as M. tuberculosis N-acetylglucosamine-1-phosphate uridyltransferase (GlmU ) inhibitors to overcome the problem of the MDR-TB. Amongst the synthesized compounds, two of them were observed to be the effective compounds of the series (IC =6.4 μM (H37Rv), MIC=25 μM (MDR-TB) and IC =2.9 μM (H37Rv), MIC=6.25 μM (MDR-TB), respectively).
耐药性结核病是一项极具挑战性的任务，迫切需要开发新的抗结核药物，这些药物应通过新型作用模式发挥作用。在这里，我们报告了 4-氨基喹唑啉作为结核分枝杆菌 N-乙酰氨基葡萄糖-1-磷酸尿苷基转移酶（GlmU）抑制剂，以克服耐多药结核病的问题。在所合成的化合物中，有两种被观察到是该系列中的有效化合物（IC=6.4μM（H37Rv），MIC=25μM（MDR-TB）和 IC=2.9μM（H37Rv），MIC=6.25μM（MDR-TB），分别）。
Zotero 插件