Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
复制标题
新型 2-芳基烷硫基-4-氨基-6-苄基嘧啶作为有效 HIV-1 非核苷逆转录酶抑制剂的合成和生物学评价
DOI：
10.1016/j.bmcl.2009.04.051
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发表时间：
2010-05-01
影响因子：
2.7
通讯作者：
Liu, Junyi
中科院分区：
文献类型：
--
作者：
Qin, Hua;Liu, Chang;Liu, Junyi
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.
