Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Synthesis, Analgesic and Anti-inflammatory Activities of 3-Ethyl-2-substituted Amino-3H-quinazolin-4-ones

R V Sheorey¹, A Thangathiruppathy², V Alagarsamy³

¹Department of Pharmacy, Karpagam University, Eachanari Post, Coimbatore â€“ 641 021; ²Department of Pharmacology, SB College of Pharmacy, Sivakasi â€“ 626 130, Tamilnadu State; ³Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy, Gr. Hyderabad -502 294, Andrapradesh State, India.

For correspondence:- V Alagarsamy Email: drvalagarsamy@gmail.com Tel:+918455230690

Received: 24 May 2012 Accepted: 10 June 2013 Published: 23 August 2013

Citation: Sheorey RV, Thangathiruppathy A, Alagarsamy V. Synthesis, Analgesic and Anti-inflammatory Activities of 3-Ethyl-2-substituted Amino-3H-quinazolin-4-ones. Trop J Pharm Res 2013; 12(4):583-589 doi: 10.4314/tjpr.v12i4.21

© 2013 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

Purpose: To synthesize a series of novel 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones and evaluate them for their analgesic and anti-inflammatory activities.

Methods: The compounds, 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones, were synthesized by reacting the amino group of 3-ethyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The synthesized compounds were characterized by Fourier transform infrared (FTIR), proton-nuclear magnetic resonance spectroscopy (¹H-NMR) and mass spectrometry. The purity of the compounds was determined by elemental analysis. Test for analgesic activity was performed by tail-flick technique using Wistar albino mice while anti-inflammatory activity was evaluated by carrageenan-induced paw oedema test in rats. Diclofenac sodium was used as positive control for both analgesic and anti-inflammatory activities.

Results: The compound, 3-ethyl-2-(cyclohexylidene-hydrazino)-3H-quinazolin-4-one (AS1), emerged as the active analgesic (activity, 63.89 %) and anti-inflammatory (activity, 60.00 %) compound of the series, and compared well with the reference standard, diclofenac sodium, which exbited analgesic and anti-inflammatory activities of 62.04 and 65.11 %, respectively.

Conclusion: The compound (AS1) can serve as a lead molecule for further development to a clinically useful novel class of analgesic and anti-inflammatory agents.

Keywords: Quinazoline, Analgesic, Anti-inflammatory, Synthesis