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在微波辐射条件下合成了系列C-2或N-3位含酯基的噻唑烷-4-酮衍生物,经水解或还原得到含亲水基如羧基、羟基的衍生物.化合物通过艾滋病毒逆转酶(HIV-RT)试剂盒(比色法)评价了其酶抑制活性.活性结果表明,部分化合物如8a,8b,9a,9b和14c能有效地抑制HIV逆转酶的活性.其中在N-3嘧啶环5位连有乙基的化合物8a和9a的活性最高,IC50值分别为3.02和3.06μmol·L-1.构效关系表明亲水性基团的引入对HIV逆转录酶抑制活性影响不大,而N-3位嘧啶基更有利于噻唑烷-4-酮抗HIV活性.
A series of thiazolidin-4-one derivatives containing ester group at C-2 or N-3 were synthesized under microwave irradiation and hydrolyzed or reduced to obtain derivatives containing hydrophilic groups such as carboxyl group and hydroxyl group. The activity of HIV-RT was evaluated by enzyme-linked immunosorbent assay (HIV-RT) kit.The activity results showed that some compounds such as 8a, 8b, 9a, 9b and 14c could effectively inhibit the activity of HIV reverse transcriptase, -3 pyrimidine ring 5-linked compounds 8a and 9a highest activity, IC50 values were 3.02 and 3.06μmol·L-1 structure-activity relationship shows that the introduction of hydrophilic groups on HIV reverse transcriptase inhibitory activity Little effect, while N-3 pyrimidinyl is more conducive to thiazolidin-4-one anti-HIV activity.