【摘 要】
：
HIV-1 non-nucleoside reverse transcriptase inhibitors(NNRTIs) play important role in the currently clinical AIDS therapies because of their potency and specificity.However,the efficacy of NNRTIs is se
【机 构】
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Department of Medicinal Chemistry,School of Pharmaceutical Sciences,Shandong University,44 West Cult
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
HIV-1 non-nucleoside reverse transcriptase inhibitors(NNRTIs) play important role in the currently clinical AIDS therapies because of their potency and specificity.However,the efficacy of NNRTIs is seriously hampered by the emergence of mutant viral strains.Therefore,it is imperative to discover new chemical entities with broad-spectrum against a variety of clinically relevant mutant,low cytotoxicity and good pharmaceutical kinetics.Recently,several 2,3-diaryl-1,3-thiazolidin-4-ones have been proved to be one of the effective NNRTIs.Structure activity relationship (SAR) studies have shown that the anti-HIV activity strongly depended on the nature of substituents at C-2 and N-3 of the thiazolidinone ring.In particular,a high activity level was found for compounds possessing a 2,6-dihalophenyl group at C-2 and a pyridin-2-yl ring at N-3.Additionally,the thiocarboxanilide UC-781 is a very potent and selective HIV-1NNRTI with a favorable resistant spectrum.Considering the complementary in structures of 2,3-diaryl-1,3-thiazolidin-4-ones and UC-781,we designed a new series of active NNRTIs based on the molecular hybridization principle.
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