Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors
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DOI：
10.1016/j.bmcl.2006.05.073
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发表时间：
2006-08-15
影响因子：
2.7
通讯作者：
He, Yun
中科院分区：
文献类型：
--
作者：
Ellis, David;Kuhen, Kelli L.;He, Yun
使用基于结构的方法发现了一系列新的喹诺酮类药物作为HIV-1非核苷类逆转录酶抑制剂（NNRTIs）。喹诺酮类铅在HIV-1复制试验中表现出个位数纳摩尔效价。通过系统的结构修饰，初步确定了这些喹诺酮类药物的合成孔径。这些新型强效喹诺酮类药物可作为进一步优化的先导药物。(c) 2006 Elsevier Ltd.版权所有。
A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization. (c) 2006 Elsevier Ltd. All rights reserved.