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…

Index: 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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Citation Number: 2

Abstract

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 ...