Synthesis and antiinflammatory activity of heterocyclic indole derivatives.
Chalcones of indole 1-5 and their corresponding products; pyrazolines 6-10 and azo compounds 11-15 were synthesised and evaluated for their antiinflammatory activity against carrageenan induced oedema in albino rats at a dose of 50 mg x kg(-1) oral. The structure of compounds was confirmed by IR, (1)H-NMR and mass spectral data. All the compounds of this series showed promising antiinflammatory activity. The most active compound of this series is 3-[1-acetyl-5-(p-hydroxyphenyl)-2-pyrazolin-3-yl]indole (7) was found to be most potent, which has shown higher percent of inhibition of oedema, lower ulcerogenic liability and acute toxicity than the standard drug phenylbutazone.
Rani
Preeti
P
Department of Pharmacology, LLRM Medical College, Meerut, U.P.-250004, India.
Srivastava
V K
VK
Kumar
Ashok
A
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan / Q000037:antagonists & inhibitors; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000188:drug therapy; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced; D023382:Toxicity Tests, Acute
D000893:Anti-Inflammatory Agents; D006571:Heterocyclic Compounds; D007211:Indoles; D002351:Carrageenan