Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
Compounds having isothiourea or thiourea functional group have shown high anti-HIV-1 activity. Therefore, a series of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones were designed, synthesized, and evaluated for anti-HIV-1 RT activity. The results of in vitro tests showed that the compound 9 exhibited EC50 at 0.26 microM with minimal toxicity in MT-4 cells as compared to 0.35 microM for thiazobenzimidazole (TBZ). It may be inferred from the present data that majority of compounds in this series exhibit higher selectivity index than TBZ.
Rawal
Ravindra K
RK
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
Tripathi
Rajkamal
R
Katti
S B
SB
Pannecouque
Christophe
C
De Clercq
Erik
E
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D053778:Thiazolidines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
D019380:Anti-HIV Agents; D053778:Thiazolidines