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.

Graphical abstractA number of amidine (2a–i) and amide (3a–h) derivatives of 3,4-diaryl-2-imino-4-thiazolines have been synthesized and screened for anti-inflammatory and analgesic activity. Compounds 2e and 3g exhibited good anti-inflammatory activity (49% and 34%, respectively) at 50 mg/kg p.o.Figure optionsDownload full-size imageDownload as PowerPoint slide