Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Rajamaki, Suvi¹  Innitzer, Anna¹  Falciani, Chiara¹  Tintori, Cristina¹  Christ, Frauke²  Witvrouw, Myriam²  Debyser, Zeger²  Massa, Silvio¹  Botta, Maurizio¹ 

[1] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[2] Katholieke Univ Leuven, B-3000 Louvain, Belgium

关键词: HIV-1;    Integrase inhibitors;    SAR study;    Thiobarbituric acid;    Rhodanine;    Thiohydantoin;   

DOI  :  10.1016/j.bmcl.2009.04.132

来源: Elsevier

【 摘 要 】

A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and cellular assays. (C) 2009 Elsevier Ltd. All rights reserved.

【 授权许可】

Free