期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 10, 页码 1699-1703出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.04.049
关键词
HIV; NNRTIs; SG-1; Structure-activity relationship; NNRTI-resistant
资金
- National Natural Basic Research Program of China [81473256, 81273561]
- Chinese Academy of Medical Sciences (CAMS) Innovation Fund for Medical Sciences [2016-I2M-1-014, 2016-I2M-3-009]
- Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study [BZ0150]
- National Science and Technology Major Project [2015ZX09102-023-004]
- Science and Technology Program of Beijing [Z151100000115008]
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.
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