期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 102, 期 -, 页码 167-179出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.07.043
关键词
HIV-1; NNRTIs; Arylthioacetanilides; SARs; Drug design; Drug-resistance
资金
- Key Project of National Natural Science Foundation of China (NSFC) for International Cooperation [81420108027, 30910103908]
- National Natural Science Foundation of China [81273354]
- Research Fund for the Doctoral Program of Higher Education of China [20110131130005]
- Natural Science Foundation of Shandong Province [ZR2009CM016]
- Science and Technology Development Project of Shandong Province [2012GSF11804]
The poor pharmacokinetics, side effects and particularly the rapid emergence of drug resistance compromise the efficiency of the clinically used anti-HIV drugs. Therefore, the discovery of novel and effective NNRTIs is still an extremely primary mission. Arylthioacetanilide family is one of the highly active HIV-1 NNRTIs against wide-type (WT) HIV-1 and a wide range of drug-resistant mutant strains. Especially, VRX-480773 and RDEA806 have been chosen as candidates for further clinical studies. In this article, we review the discovery and development of the arylthioacetanilides, and, especially, pay much attention to the structural modifications, SARs conclusions and molecular modeling. Moreover, several medicinal chemistry strategies to overcome drug resistance involved in the optimization process of arylthioacetanilides are highlighted, providing valuable clues for further investigations. (C) 2015 Elsevier Masson SAS. All rights reserved.
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