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 reverse transcriptase inhibitors (NNRTIs).
Rao
Angela
A
Dipartimento Farmaco-Chimico, Università di Messina, viale Annunziata, 98168, Messina, Italy.
Balzarini
Jan
J
Carbone
Anna
A
Chimirri
Alba
A
De Clercq
Erik
E
Monforte
Anna Maria
AM
Monforte
Pietro
P
Pannecouque
Christophe
C
Zappalà
Maria
M
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004353:Drug Evaluation, Preclinical; D015497:HIV-1 / Q000187:drug effects / Q000254:growth & development; D015498:HIV-2 / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects / Q000821:virology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D013844:Thiazoles