【摘 要】
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Non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been widely used in the treatment of AIDS patients owing to their high selectivity,relatively low toxicity and potent activity.DABO(Dihydro
【机 构】
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School of Pharmaceutical Sciences,Shandong University,44 West Culture Road,250012,Jinan,Shandong
【出 处】
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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
Non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been widely used in the treatment of AIDS patients owing to their high selectivity,relatively low toxicity and potent activity.DABO(Dihydro-alkoxyl-benzyl-oxopyrimidine) and DAPY(Diaryl pyrimidines) analogues represented two important and promising classes of HIV-1 NNRTIs.Based on the structural features,binding mode and SAR study of these two pyrimidine-based NNRTIs,we made several modifications in the nucleus ring and their substituents according to the bioisosterism principle,and designed,synthesized two series of 1,2,6-thiadiazine-l,l-dione derivatives(Ⅰa-Ⅰx & Ⅱa-Ⅱz,totally 50 compounds) with an attempt to improve the hydrogen bond between the ligands and RT.15 specifically chosen compounds were evaluated for their anti-RT activity.The results indicated that these compounds showed a wide range of activities.
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