title: Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity.
abstract: A novel series of synthetic 2'-hydroxychalcones (1a-h), 2'-methoxychalcones (2a-l), flavanones (3a-k) and flavones (4a-f) have been synthesized and evaluated for their anti-inflammatory activity in carrageenan induced rat paw oedema model. Compounds 1a, 1e-g, 2e-g, 3j, and 4f showed potent anti-inflammatory activity comparable to the reference drug indomethacin with insignificant ulceration. Compound 1f showed mild inhibition against the enzymatic activity of ovine COX-1 and COX-2 (in-vitro). Compound 1f also exhibited inhibitory activity in LPS induced TNF-α production.
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Sameena
authors.initials: S
authors.lastname: Bano
authors.forename: Kalim
authors.initials: K
authors.lastname: Javed
authors.forename: Shamim
authors.initials: S
authors.lastname: Ahmad
authors.forename: I G
authors.initials: IG
authors.lastname: Rathish
authors.forename: Surender
authors.initials: S
authors.lastname: Singh
authors.forename: M
authors.initials: M
authors.lastname: Chaitanya
authors.forename: K M
authors.initials: KM
authors.lastname: Arunasree
authors.forename: M S
authors.initials: MS
authors.lastname: Alam
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D002460:Cell Line; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005260:Female; D044950:Flavanones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047309:Flavones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008297:Male; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D012756:Sheep; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D047188:Chalcones; D016861:Cyclooxygenase Inhibitors; D044950:Flavanones; D047309:Flavones; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; D002351:Carrageenan; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2
keywords: Anti-inflammatory; Chalcone; Flavanone; Flavone; Indomethacin; TNF-α