Naphthyridinone (NTD) integrase inhibitors: N1 Protio and methyl combination substituent effects with C3 amide groups
Naphthyridinone (NTD) integrase inhibitors: N1 Protio and methyl combination substituent effects with C3 amide groups
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DOI：
10.1016/j.bmcl.2012.11.071
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发表时间：
2013-01-15
影响因子：
2.7
通讯作者：
Fujiwara, Tamio
中科院分区：
文献类型：
--
作者：
Johns, Brian A.;Kawasuji, Takashi;Fujiwara, Tamio
Substituent effects of a series of N1 protio and methyl naphthyridinone HIV-1 integrase strand-transfer inhibitors has been explored. The effects of combinations of the N1 substituent and C3 amide groups was extensively studied to compare enzyme inhibition, antiviral activity and protein binding effects on potency. The impact of substitution on ligand efficiency was considered and several compounds were advanced into in vivo pharmacokinetic studies ultimately leading to the clinical candidate GSK364735. (C) 2012 Elsevier Ltd. All rights reserved.
