Dollé V, Fan E, Nguyen C H, Aubertin A M, Kirn A, Andreola M L, Jamieson G, Tarrago-Litvak L, Bisagni E
URA 1387 CNRS, Synthèse Organique, Institut Curie, Section de Recherche, Orsay, France.
J Med Chem. 1995 Nov 10;38(23):4679-86. doi: 10.1021/jm00023a007.
4-(Arylthio)-pyridin-2(1H)-ones variously substituted in their 3-, 5-, and 6-positions have been synthesized as a new series of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone hybrid molecules. Biological studies revealed that some of them show potent HIV-1 specific reverse transcriptase inhibitory properties. Compounds 16 and 7c, the most active ones, inhibit the replication of HIV-1 at 3 and 6 nM, respectively.
在其3、5和6位上有不同取代基的4-（芳硫基）吡啶-2（1H）-酮已被合成为一系列新型的1-[(2-羟基乙氧基)甲基]-6-(苯硫基)胸腺嘧啶（HEPT）-吡啶酮杂合分子。生物学研究表明，其中一些化合物具有强效的HIV-1特异性逆转录酶抑制特性。活性最强的化合物16和7c分别在3 nM和6 nM时抑制HIV-1的复制。
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