Synthesis, Analgesic and
Anti-inflammatory Activities of 3-Ethyl-2-substituted
Amino-3H-quinazolin-4-ones
RV Sheorey1, A
Thangathiruppathy2 and V Alagarsamy3*
1Department of Pharmacy,
Karpagam University, Eachanari Post, Coimbatore – 641
021, 2Department of Pharmacology, SB College
of Pharmacy, Sivakasi – 626 130, Tamilnadu State, 3Medicinal
Chemistry Research Laboratory, MNR College of Pharmacy,
Sangareddy, Gr. Hyderabad -502 294, Andrapradesh State,
India.
*For correspondence:
Email:
drvalagarsamy@gmail.com Tel: +91
8455-230690; Fax: +91 8455-230 555;
Received: 24 May 2012
Revised accepted: 10 June 2013
Tropical Journal of
Pharmaceutical Research, August 2013; 12(4): 583-589
http://dx.doi.org/10.4314/tjpr.v12i4.21
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
