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摘要
A series of N-(3-(substituted-alkyl- or halophenyl)-4-methylthiazol-2(3H)-ylidene)-substituted alkyl- or halo-benzamides 21-40 were prepared by base-catalyzed cyclization of the corresponding 1-(substituted-alkyl- or halo-benzoyl)-3-(substituted-halophenyl)thioureas 1-20. Substituted pyrazolo[4,3-d]thiazol-5(6aH)-ylidene)benzamides 45a-d were synthesized by cycloaddition of compound 45 with the reactive cumulene intermediates 42a-d. All compounds were evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 in MT-4. Compounds 35 and 39 showed an IC(50) of 2.02 mu g mL(-1) and 0.40 mu g mL(-1) against the HIV-2 strain ROD with CC(50) of >= 104.00 mu g mL(-1) and > 125.00 mu g mL(-1) respectively, resulting in a selectivity index of >= 52 and > 313. Based on the chemical structure of compounds 35 and 39, these molecules can be proposed to act as NNRTIs. However, it is exceptional to observe an antiretroviral activity that is limited to HIV-2.
- 出版日期2011-5
- 单位河北医科大学
