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学科主题: 药学
题名:
Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
作者: Qin, Hua2; Liu, Chang2; Zhang, Jianfang2; Guo, Ying1; Zhang, Siwei3; Zhang, Zhili1; Wang, Xiaowei1; Zhang, Liangren3; Liu, Junyi1,3
关键词: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) ; 2-Aryalkylthio-4-amino-6-benzylpyrimidines ; Docking
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2010-05-01
DOI: 10.1016/j.bmcl.2009.04.051
卷: 20, 期:9, 页:3003-3005
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: STRUCTURE-BASED DESIGN ; ANTI-HIV-1 ACTIVITY ; POSITIONAL ADAPTABILITY ; CONFORMATIONAL-CHANGES ; DERIVATIVES ; SERIES ; BINDING
英文摘要:

Novel 2-aryalkylthio-4-amino-6-benzylpyrimidines (3a-i), which can be considered as S-DABO and TMC-125 analogue hybrid molecules, have been designed and synthesized as inhibitors of HIV-1 RT. The results clearly indicated that the changes at the N(3)/C(4) position of pyrimidine ring could affect the hydrogen bonds strength and number between N(3)/C(4) and the Lys101 residue which are indispensable for anti-HIV-1 RT activity. The biological activity results are also in accordance with the docking study. (C) 2009 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 20672008
项目资助者: National Sciences Foundation of China ; Ministry of Education of China
WOS记录号: WOS:000276816600068
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62905
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, State key Lab Natl & Biomimet Drug, Beijing 100191, Peoples R China

Recommended Citation:
Qin, Hua,Liu, Chang,Zhang, Jianfang,et al. Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(9):3003-3005.
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