title: Synthesis and evaluation of analgesic and anti-inflammatory activities of most active free radical scavenging derivatives of embelin-A structure-activity relationship.
abstract: Antioxidant and related properties of the plant Embelia ribes and embelin are well known. In the present study embelin was condensed with various aromatic substituted primary amines to yield ten new and one reported derivatives along with monomethyl embelin. All these compounds along with embelin were evaluated for in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picryl hydrazyl (DPPH) methods. Two para-substituted embelin derivatives showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and both of its derivatives almost completely abolished the acetic acid induced writhing. p-Sulfonylamine phenylamino derivative showed better anti-inflammatory activity than embelin.
authors.affiliation: Department of Pharmaceutical Chemistry, J.S.S. College of Pharmacy, Rocklands, Ootacamund, TN, India. mahendransekar_05@yahoo.co.in
authors.forename: Sekar
authors.initials: S
authors.lastname: Mahendran
authors.forename: Shrishailappa
authors.initials: S
authors.lastname: Badami
authors.forename: Subban
authors.initials: S
authors.lastname: Ravi
authors.forename: Boreddy Shivanandappa
authors.initials: BS
authors.lastname: Thippeswamy
authors.forename: Veeresh Prabhakar
authors.initials: VP
authors.lastname: Veerapur
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D016227:Benzoquinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D052160:Benzothiazoles / Q000737:chemistry; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D031645:Embelia / Q000737:chemistry*; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D005638:Fruit / Q000737:chemistry; D006614:Hindlimb / Q000187:drug effects; D051379:Mice; D010146:Pain / Q000188:drug therapy; D010936:Plant Extracts / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship; D013451:Sulfonic Acids / Q000737:chemistry
chemical_list: D000893:Anti-Inflammatory Agents; D016227:Benzoquinones; D052160:Benzothiazoles; D016166:Free Radical Scavengers; D010936:Plant Extracts; D013451:Sulfonic Acids; C002502:2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid; C010945:embelin