Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors

On the basis of QSAR-based drug design strategy and bioisosteric principle, a series of novel thiazolidin-4-ones bearing different aryl/heteroaryl moieties at position C-2 and N-3 of thiazolidin-4-one were synthesized and evaluated as potent inhibitors of human immunodeficiency virus type-1 (HIV-1).