A NOVEL APPROACH TOWARDS DEVELOPMENT OF QUINAZOLINE DERIVATIVES IN PAIN MANAGEMENT
Objective: To synthesis evaluation of the analgesic and anti-inflammatory activities of pyrazoline bearing 4(3H)-quinazolinone derivatives.
Methods: Synthesis of Chalcone (3a-3j) involves the Claisen-Schmidt condensation of equimolar quantities of substituted acetophenone with aromatic aldehyde in the presence of aqueous alkali (10%). Comp. (3a-3j) undergoes cyloaddition reaction with semicarbazide HCl in the presence of suitable solvent to yield comp. (4a-4j). It undergoes addition cyclization reaction with anthranillic acid to yield final comp. (6a-6j). Acute toxicity study of synthesized compound was found according to OECD guidelines 423. The test compound do not showed any toxicity up to 200mg/kg dose. Mortality was not observed during the course of study. The analgesic and anti-inflammatory activity of all synthesized compounds were carried by using hot plate method and Carrageenan induced Rat Paw Edema Method respectively.
Results: All compounds synthesized are obtained in crystalline form with good practical yield. The purity and homogeneity of compounds synthesized were determined by sharp melting points and TLC method. The chemical structures were confirmed by FTIR, 1HNMR, and Mass spectrum.
Conclusion: The synthesized compound 6b, 6d, 6e, 6i and 6j showed good analgesic and anti-inflammatory activities whereas others showed significant activities.
Keywords: Quinazoline, pyrazole, analgesic and anti-inflammatory activity.
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