Design and synthesis of N1-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

被引：49
|
作者：
Monforte, Anna-Maria [1 ]
Ferro, Stefania [1 ]
De Luca, Laura [1 ]
Lo Surdo, Giuseppa [1 ]
Morreale, Francesca [1 ]
Pannecouque, Christophe [2 ]
Balzarini, Jan [2 ]
Chimirri, Alba [1 ]
机构：
[1] Univ Messina, Dipartimento Sci Farmaco & Prod Salute, I-98168 Messina, Italy
[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 04期
关键词：
HIV-1 reverse transcriptase; NNRTIs; N-1-Aryl-benzimidazoles; 2-substituted; Synthesis; IMMUNODEFICIENCY-VIRUS TYPE-1; WILD-TYPE; POTENT; DISCOVERY; ANALOGS; UPDATE;
D O I：
10.1016/j.bmc.2013.12.045
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of novel N-1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1459 / 1467
页数：9
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