Synthesis and QSAR studies on thiazolidinones as anti-HIV agents.
Selected 4-thiazolidinone have been synthesized and tested as anti-HIV activity. The results of the in vitro tests showed that one of the compounds, 5, inhibited the enzyme at 0.204 microM concentration with minimal toxicity to MT-4 cell. Furthermore, the QSAR studies indicated the role of PMIZ, Ovality and Total energy content of the compounds in rationalizing the activity.
Rawal
Ravindra K
RK
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
Solomon
V Raja
VR
Prabhakar
Yenamandra S
YS
Katti
S B
SB
De Clercq
E
E
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000737:chemistry / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008956:Models, Chemical; D021281:Quantitative Structure-Activity Relationship; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000494:pharmacology*; D018675:Toxicity Tests; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D018894:Reverse Transcriptase Inhibitors; D045162:Thiazolidinediones; D054303:HIV Reverse Transcriptase