Non-nucleoside reverse transcriptase inhibitors (NNRTIs) represent potent anti-HIV agents targeting HIV-1 reverse transcriptase (RT), a crucial enzyme for the viral life cycle. We have previously identified a series of NNRTIs bearing a 2,3-diaryl-1,3-thiazolidin-4-one core and some compounds proved to be effective in inhibiting HIV-1 replication at micromolar concentration. As a continuation in this research work we report the design, the synthesis and the structure–activity relationship studies of a further series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives containing an arylthioacetamide group as pharmacophoric structural requirement for binding to the RT catalytic area. The new compounds proved to be effective to inhibit RT activity at micromolar concentrations. Finally, docking studies were carried out in order to rationalize the biological results of the new synthesized inhibitors.

非核苷逆转录酶抑制剂（NNRTIs）代表针对HIV-1逆转录酶（RT）的有效抗HIV药物，RT-1是病毒生命周期的关键酶。我们先前已经确定了一系列带有2,3-二芳基-1,3-噻唑烷-4-酮核心的NNRTI，并且一些化合物被证明可有效抑制微摩尔浓度的HIV-1复制。作为这项研究的继续，我们报告了进一步的含芳硫基乙酰胺的3-（1,3,4-噻二唑-2-基）噻唑烷丁-4-酮衍生物的设计，合成和结构-活性关系的研究该基团是结合到RT催化区域的药效学结构要求。新化合物被证明可有效抑制微摩尔浓度的RT活性。最后，