Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30–50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 r...

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Veröffentlicht in:	Farmaco (Società chimica italiana : 1989) 2004, Vol.59 (1), p.33-39
Hauptverfasser:	Rao, Angela, Balzarini, Jan, Carbone, Anna, Chimirri, Alba, De Clercq, Erik, Monforte, Anna Maria, Monforte, Pietro, Pannecouque, Christophe, Zappalà, Maria
Format:	Artikel
Sprache:	eng
Schlagworte:	2,3-diaryl-1,3-thiazolidin-4-ones Anti-HIV activity Anti-HIV Agents - chemical synthesis Anti-HIV Agents - pharmacology Cell Survival - drug effects Cell Survival - physiology Drug Evaluation, Preclinical HIV-1 - drug effects HIV-1 - growth & development HIV-2 - drug effects HIV-2 - growth & development Humans Molecular Structure NNRTIs Reverse Transcriptase Inhibitors - chemical synthesis Reverse Transcriptase Inhibitors - pharmacology Structure-Activity Relationship T-Lymphocytes - drug effects T-Lymphocytes - virology Thiazoles - chemical synthesis Thiazoles - pharmacology Virus Replication - drug effects
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Zusammenfassung:	Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30–50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).
ISSN:	0014-827X 1879-0569
DOI:	10.1016/j.farmac.2003.09.001