European Journal of Medicinal Chemistry p. 309 - 316 (2016)
Update date:2022-08-04
Topics:
Xu, Zhongliang
Guo, Jiamei
Yang, Ying
Zhang, Mengdi
Ba, Mingyu
Li, Zhenzhong
Cao, Yingli
He, Ricai
Yu, Miao
Zhou, Hua
Li, Xiaoxi
Huang, Xiaoshan
Guo, Ying
Guo, Changbin
In our previous work, novel 2,4,5-trisubstituted thiazole derivatives (TSTs) were synthesized, and their activities were evaluated against HIV-1 reverse transcriptase. Some interesting results were obtained, which led us to a new discovery regarding these TSTs. In the present study, 21 new 2,4,5-trisubstituted thiazole derivatives were rationally designed and synthesized as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) in accordance with our previous study. Among the synthesized target compounds, compounds 14, 16, 17, and 19 showed more potent inhibitory activities against HIV-1 with an IC50value of 0.010?μM. Compounds 4, 9, 10, 11, 13 and 16 were further tested on nine NNRTI-resistant HIV-1 strains, and all of these compounds exhibited inhibitory effects. A molecular docking study was conducted, and the results showed a consistent and stable binding mode for the typical compounds. These results have provided deeper insights and SAR of these types of NNRTIs.
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