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3.06 μmol·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 possessing ester were synthesized under microwave irradiation, and then the corresponding products with hydrophilic groups, like carboxyl and hydroxyl groups, were obtained after hydrolysis reaction or reduction reaction. The compounds were evaluated for their human immunodeficiency virus (HIV) reverse transcriptases inhibitory activities in vitro HIV-RT kit assay (colorimetric method). The results showed that some of the compounds, such as 8a, 8b, 9a, 9b and 14c, could effectively inhibit RT activity. Among them, compounds 8a and 9a where ethyl group existed at 5-position on N-3 pyrimidine ring were the best ones with the IC₅₀ values of 3.02 and 3.06 μmol·L^-1, respectively. Structure activity relationship analysis of these analogues suggested that the introduction of hydrophilic groups had little effect on their anti-HIV-RT activity and the N-3 pyrimidine moiety on thiazolidin-4-one ring should be more favorable to the anti-HIV activity than the C-2 phenyl group.