Arylamide inhibitors of HIV-1 integrase

…, N Neamati, A Mazumder, S Sunder…

Index: Zhao, He; Neamati, Nouri; Mazumder, Abhijit; Sunder, Sanjay; Pommier, Yves; Burke Jr., Terrence R. Journal of Medicinal Chemistry, 1997 , vol. 40, # 8 p. 1186 - 1194

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Citation Number: 105

Abstract

Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency. The ability of such catechol species to undergo in situ oxidation to reactive quinones presents one potential limitation to their utility. In an effort to ...