Exploring MDR‐TB inhibitory potential of 4‐amino quinazolines as Mycobacterium tuberculosisN ‐acetylglucosamine‐1‐phosphate uridyltransferase (GlmU MTB) inhibitors,Chemistry & Biodiversity

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Exploring MDR‐TB inhibitory potential of 4‐amino quinazolines as Mycobacterium tuberculosisN ‐acetylglucosamine‐1‐phosphate uridyltransferase (GlmU MTB) inhibitors
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-07-20 , DOI: 10.1002/cbdv.202000237
Harun M Patel _{1,

2} , Mahesh Palkar ₁ , Rajshekhar Karpoormath ₁

Affiliation

Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new anti-tubercular agents which operate via novel modes of action. Here, we are reporting the 4-amino quinazolines as M. tuberculosis N -acetylglucosamine-1-phosphate uridyltransferase (GlmU MTB) inhibitors to overcome the problem of the MDR-TB. Amongst the synthesized compounds HMP-05 and HMP-15 was observed to be the effective compound of the series [IC 50 = 6.4 µM (H37Rv), MIC = 25 µM (MDR-TB) and IC 50 = 2.9 µM (H37Rv), MIC = 6.25 µM (MDR-TB) respectively].

中文翻译：

探索 4-氨基喹唑啉作为结核分枝杆菌 N-乙酰氨基葡萄糖-1-磷酸尿苷转移酶 (GlmU MTB) 抑制剂的 MDR-TB 抑制潜力

耐药结核病是一项具有挑战性的任务，迫切需要开发通过新型作用方式起作用的新型抗结核药物。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-磷酸尿苷转移酶 (GlmU MTB) 抑制剂，以克服 MDR-TB 的问题。在合成的化合物中，观察到 HMP-05 和 HMP-15 是该系列的有效化合物 [IC 50 = 6.4 µM (H37Rv)，MIC = 25 µM (MDR-TB) 和 IC 50 = 2.9 µM (H37Rv)， MIC = 6.25 µM (MDR-TB) 分别]。

更新日期：2020-07-20

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