Design, synthesis and biological evaluation of substituted (+)-SG-l derivatives as novel anti-HIV agents
Design, synthesis and biological evaluation of substituted (+)-SG-l derivatives as novel anti-HIV agents
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新型抗 HIV 药物取代 ( )-SG-1 衍生物的设计、合成和生物学评价
DOI：
10.1016/j.bmcl.2018.04.049
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发表时间：
2018-06-01
影响因子：
2.7
通讯作者：
Xie, Ping
中科院分区：
文献类型：
--
作者：
Liu, Xiaoyu;Chen, Panpan;Xie, Ping
SG-1 was previously identified as a potent Non-nucleoside reverse transcriptase inhibitors (NNRTI) which works through inhibition of reverse transcriptase (RT) RNA-dependent DNA polymerase activity via a direct binding event. To further investigate the relationship between its structure and activity, four series of novel analogues were designed and synthesized with 12 of them inhibiting HIV-1 replication with IC(50)s in the range 0.09-6.71 mu M. Compound 4b, 4c, 4f, 2 and 6b were further tested on two NNRTI-resistant HIV-1 strains and one NNRTI-resistant superbug. The result showed that RT- E138K/M184V mutant virus conferred 4.7-9.1-fold resistance to 4c, 4f, 2 and 6b, but only showed slight resistance to 4b (2-fold) which was better than SG-1. (C) 2018 Elsevier Ltd. All rights reserved.
