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Analogs of N′-hydroxy-N-(4H, 5H-naphtho [1, 2-d] thiazol-2-yl) methanimidamide inhibit Mycobacterium tuberculosis methionine aminopeptidases

S Bhat, O Olaleye, KJ Meyer, W Shi, Y Zhang…

文献索引:Bhat, Shridhar; Olaleye, Omonike; Meyer, Kirsten J.; Shi, Wanliang; Zhang, Ying; Liu, Jun O. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 14 p. 4507 - 4513

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被引用次数: 2

摘要

Our previous target validation studies established that inhibition of methionine aminopeptidases (MtMetAP, type 1a and 1c) from Mycobacterium tuberculosis (Mtb) is an effective approach to suppress Mtb growth in culture. A novel class of MtMetAP1c inhibitors comprising of N′-hydroxy-N-(4H, 5H-naphtho [1, 2-d] thiazol-2-yl) methanimidamide (4c) was uncovered through a high-throughput screen (HTS). A systematic structure–activity ...