Synthesis of amidine and amide derivatives and their evaluation for anti-inflammatory and analgesic activities.
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.
Sondhi
Sham M
SM
Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, Uttarakhand, India. sondifcy@iitr.ernet.in
Singh
Jaiveer
J
Kumar
Ashok
A
Jamal
Hyder
H
Gupta
P P
PP
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
D000577:Amides; D000578:Amidines; D000700:Analgesics; D000893:Anti-Inflammatory Agents