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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.
Afiliación
  • Xu Z; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Guo J; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
  • Yang Y; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
  • Zhang M; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Ba M; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
  • Li Z; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Cao Y; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
  • He R; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Yu M; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
  • Zhou H; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Li X; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Huang X; Department of Chemistry, Capital Normal University, Beijing, 100048, China.
  • Guo Y; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China. Electronic address: yingguo6@imm.ac.cn.
  • Guo C; Department of Chemistry, Capital Normal University, Beijing, 100048, China. Electronic address: guocb@cnu.edu.cn.
Eur J Med Chem ; 123: 309-316, 2016 Nov 10.
Article en En | MEDLINE | ID: mdl-27484516
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 IC50 value 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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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiazoles / VIH-1 / Inhibidores de la Transcriptasa Inversa / Transcriptasa Inversa del VIH / Mutación Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2016 Tipo del documento: Article País de afiliación: China Pais de publicación: Francia
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiazoles / VIH-1 / Inhibidores de la Transcriptasa Inversa / Transcriptasa Inversa del VIH / Mutación Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2016 Tipo del documento: Article País de afiliación: China Pais de publicación: Francia