BIOMAT Database Logo BIOMAT Database Logo

Recent advances in the research of 2,3-diaryl-1,3-thiazolidin-4-one derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. 2012

Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, PR China.

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.

UI MeSH Term Description Entries
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D053778 Thiazolidines Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES. Thiazolidine
D054303 HIV Reverse Transcriptase A reverse transcriptase encoded by the POL GENE of HIV. It is a heterodimer of 66 kDa and 51 kDa subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse H activity (RIBONUCLEASE H, HUMAN IMMUNODEFICIENCY VIRUS) that plays an essential role the viral replication process. Reverse Transcriptase, HIV,Reverse Transcriptase, Human Immunodeficiency Virus,Transcriptase, HIV Reverse
D055808 Drug Discovery The process of finding chemicals for potential therapeutic use. Drug Prospecting,Discovery, Drug,Prospecting, Drug
D018894 Reverse Transcriptase Inhibitors Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. Reverse Transcriptase Inhibitor,Inhibitors, Reverse Transcriptase,Inhibitor, Reverse Transcriptase,Transcriptase Inhibitor, Reverse

Related Publications

Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Recent advances of diaryl ether family as HIV-1 non-nucleoside reverse transcriptase inhibitors.
January 2013, Current pharmaceutical design,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Recent advances in the DABOs family as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
January 2011, Current medicinal chemistry,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Novel Thiazolidin-4-ones as Potential Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase.
October 2019, Molecules (Basel, Switzerland),
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents.
July 2001, Bioorganic & medicinal chemistry letters,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
August 2004, Antiviral research,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
June 2015, European journal of medicinal chemistry,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.
September 2002, Farmaco (Societa chimica italiana : 1989),
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Structural Basis of 2-Phenylamino-4-phenoxyquinoline Derivatives as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
January 2022, Molecules (Basel, Switzerland),
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Non Nucleoside Reverse Transcriptase Inhibitors, Molecular Docking Studies and Antitubercular Activity of Thiazolidin-4-one Derivatives.
January 2019, Current computer-aided drug design,
Ye Tian, and Peng Zhan, and Diwakar Rai, and Jiyan Zhang, and Erik De Clercq, and Xinyong Liu
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
June 2014, Bioorganic & medicinal chemistry,
Copied contents to your clipboard!