A NOVEL APPROACH TOWARDS DEVELOPMENT OF QUINAZOLINE DERIVATIVES IN PAIN MANAGEMENT


Niraj Kumar Sudheshwar Sinha, Alpana J Asnani, Bhushanr R Dravyaka

Abstract


ABSTRACT-

 

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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About this article

Title

A NOVEL APPROACH TOWARDS DEVELOPMENT OF QUINAZOLINE DERIVATIVES IN PAIN MANAGEMENT

Date

01-08-2013

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 6 Suppl 3 (July-Sept) 2013 Page: 200-204

Print ISSN

0974-2441

Online ISSN

2455-3891

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349 Views | 164 Downloads

Authors & Affiliations

Niraj Kumar Sudheshwar Sinha
R. T. M. Nagpur University Nagpur
India

Alpana J Asnani
R. T. M. Nagpur University
India

Bhushanr R Dravyaka
India


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