Development of isoniazid–NAD truncated adducts embedding a lipophilic fragment as potential bi-substrate InhA inhibitors and antimycobacterial agents

…, V Bernardes-Génisson, A Quémard, P Constant…

Index: Delaine, Tamara; Bernardes-Genisson, Vania; Quemard, Annaik; Constant, Patricia; Meunier, Bernard; Bernadou, Jean European Journal of Medicinal Chemistry, 2010 , vol. 45, # 10 p. 4554 - 4561

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Citation Number: 36

Abstract

Isoniazid-NAD truncated adducts embedding a lipophilic fragment were designed, synthesized and evaluated as inhibitors of the enoyl-acyl carrier protein (ACP) reductase (InhA) of Mycobacterium tuberculosis and as antimycobacterial agents. These compounds, planned as bi-substrate inhibitors and inspired from the active metabolite of isoniazid, combine both the nicotinamide moiety of the cofactor NAD and a lipophilic hydrocarbon ...