title: Structure-based rationale design and synthesis of aurantiamide acetate analogues - towards a new class of potent analgesic and anti-inflammatory agents.
abstract: A series of new aurantiamide acetate analogues were synthesized by modifying its N-terminal substitution and the amino acid residue. The structure of all these compounds was established on the basis of analytical and spectral studies. All the new derivatives were evaluated in vivo for their analgesic activity by tail flick method in mice and anti-inflammatory activity against carrageenan-induced oedema in albino rats at different doses (25, 50 and 100 mg/kg body weight). All the compounds exhibited significant pharmacological activity with no ulcerogenic liability. In particular, pentapeptides and tricosamers (30 amino acids) containing analogues have demonstrated high potency than the reference standards. These compounds hold promise for further development.
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore, India.
authors.forename: Ramesh
authors.initials: R
authors.lastname: Suhas
authors.forename: Dase
authors.initials: D
authors.lastname: Channe Gowda
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D002351:Carrageenan; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D008297:Male; D051379:Mice; D010146:Pain / Q000188:drug therapy; D028502:Polygonum / Q000737:chemistry*; D051381:Rats; D014456:Ulcer / Q000139:chemically induced
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D004151:Dipeptides; C011670:N-benzoylphenylalanylphenylalinol acetate; D002351:Carrageenan