title: Synthesis of amidine and amide derivatives and their evaluation for anti-inflammatory and analgesic activities.
abstract: A number of amidine derivatives (2a-i) have been synthesized by condensation of 2-cyanopyridine with various 3,4-diaryl-2-imino-4-thiazolines. Various amide derivatives (3a-h) were synthesized by condensation of orotic acid and hydantoin-5-acetic acid with a number of 3,4-diaryl-2-imino-4-thiazolines using microwave irradiation. All the compounds i.e. (2a-i) and (3a-h) synthesized were characterized by spectroscopic means and elemental analysis. Compounds (2a-i) and (3a-h) at 50 mg/kg p.o. were screened for anti-inflammatory activity whereas 2a-d, f, g, i and 3a, b, d, f at 50 mg/kg p.o. were evaluated for analgesic activity. Compounds 2e and 3g exhibited good anti-inflammatory activity (49% and 34%, respectively) and 2f, g showed interesting (50% in each case) analgesic activity.
authors.affiliation: Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, Uttarakhand, India. sondifcy@iitr.ernet.in
authors.forename: Sham M
authors.initials: SM
authors.lastname: Sondhi
authors.forename: Jaiveer
authors.initials: J
authors.lastname: Singh
authors.forename: Ashok
authors.initials: A
authors.lastname: Kumar
authors.forename: Hyder
authors.initials: H
authors.lastname: Jamal
authors.forename: P P
authors.initials: PP
authors.lastname: Gupta
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000578:Amidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D051381:Rats; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000578:Amidines; D000700:Analgesics; D000893:Anti-Inflammatory Agents