Nonnucleoside HIV-1 reverse transcriptase inhibitors: Part I. Synthesis and structure-activity relationship of 1-alkoxymethyl-5-alkyl-6-naphthylmethyl uracils as HEPT …

…, E De Clercq, J Balzarini, C Pannecouque

Index: Meng, Ge; Chen, Fen-Er; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe Chemical and Pharmaceutical Bulletin, 2003 , vol. 51, # 7 p. 779 - 789

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Citation Number: 39

Abstract

1-Alkoxymethyl-5-alkyl-6-naphthylmethyl uracils, which are novel 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues, were synthesized for evaluation as selective and potent nonnucleoside human immunodeficiency virus (HIV)-1 reverse transcriptase inhibitors. The anti-HIV-1 activity of these compounds was assayed in vitro using HIV-1 infected MT-4 and CEM bioassays. The EC 50, CC 50 and SI were recorded ...