title: Recent advances in the research of 2,3-diaryl-1,3-thiazolidin-4-one derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
abstract: Derived from the structure of 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), 2,3-diaryl-1,3-thiazolidin-4-one derivatives became a novel class of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Under the guidance of continuous structure-activity relationship (SAR) analysis and molecular modeling, various structural modifications were carried out on nearly all the positions of the thiazolidin-4-one nucleus. Some of the derivatives proved to be highly effective against HIV-1 replication at 10-40 nanomolar concentration ranges with minimal cytotoxicities. In this article, the whole development of 2,3-diaryl-1,3-thiazolidin-4-one series from the discoveries to recent advances, their panoramic SAR studies and binding modes based on molecular modeling were reviewed, and also some enlightenments for further investigation were presented.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, PR China.
authors.forename: Ye
authors.initials: Y
authors.lastname: Tian
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.forename: Diwakar
authors.initials: D
authors.lastname: Rai
authors.forename: Jiyan
authors.initials: J
authors.lastname: Zhang
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D055808:Drug Discovery / Q000379:methods*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D018894:Reverse Transcriptase Inhibitors; D053778:Thiazolidines; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase