Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity

…, V Huteau, G Marchal, H Munier-Lehmann…

Index: Gasse, Cecile; Douguet, Dominique; Huteau, Valerie; Marchal, Gilles; Munier-Lehmann, Helene; Pochet, Sylvie Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 11 p. 6075 - 6085

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Citation Number: 65

Abstract

A series of N1-(4-substituted-benzyl)-pyrimidines were synthesized as potential inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt). Key SAR parameters included the chain length substitution in para position of the benzyl ring, the functional group terminating the alkyl chain, and the substituent on the C-5 pyrimidine ring. Synthesized molecules were assayed against both recombinant enzyme and ...