1326318-99-3Relevant academic research and scientific papers
2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5
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
, p. 309 - 316 (2016)
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.
Synthesis and crystal structure of chalcones as well as on cytotoxicity and antibacterial properties
Wu, Jianzhang,Wang, Cong,Cai, Yuepiao,Peng, Jing,Liang, Donglou,Zhao, Yunjie,Yang, Shulin,Li, Xiaokun,Wu, Xiaoping,Liang, Guang
experimental part, p. 444 - 452 (2012/08/28)
A series of chalcones derivatives were synthesized and evaluated for cytotoxic and antibacterial activities in vitro. These modifications changed their bioactivity profile and indicated a combination of SAR analysis toward the substituents in rings A and
