|
|
Original Research Article
Synthesis of
1-Substituted-4-(Pyridin-4-yl) [1,2,4] Triazolo [4,3-a]
Quinazolin-5(4H)-ones as a New Class of
H1-Antihistaminic Agents
M Gobinath1*, N
Subramanian2, V Alagarsamy3, S
Nivedhitha1 and V Raja Solomon3
1Department of Pharmaceutical
Chemistry, Ratnam Institute of Pharmacy, Pidathapolur
Village, Nellore – 524 346, 2Department of
Pharmaceutical Technology, Anna University of
Technology, Tiruchirappalli – 620 024, 3Medicinal
Chemistry Research Laboratory, MNR College of Pharmacy,
Sangareddy, Gr. Hyderabad-502 294, India
*For correspondence:
Email:
drvalagarsamy@gmail.com; Tel:
+91-9246425702, 8008100003
Received: 23 January 2014
Revised accepted: 23
December 2014
Tropical Journal of Pharmaceutical Research,
February 2015;
14(2):
271-277
http://dx.doi.org/10.4314/tjpr.v14i2.12
Abstract
Purpose: To synthesize a new series
of 1-substituted-4-(pyridin-4-yl) [1,2,4]
triazolo[4,3-a]quinazolin-5(4H)-ones and evaluate them
for H1-antihistaminic activity with negligible side
effects in guinea pigs.
Methods: The synthesized compounds
were characterized by Infrared spectroscopy (IR), proton
nuclear magnetic resonance (1H-NMR) and mass
spectrometry (MS) data. The purity of the compounds was
determined by elemental analysis. The antihistaminic
activity of the compounds was evaluated in guinea pigs
by histamine-induced bronchoconstriction method.
Results: Among the series,
1-methyl-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a]
quinazolin-5(4H)-one (S5) was the most potent with 72.85
% protection and its potency was comparable to that of
the reference, chlorpheniramine maleate (70.09 %).
Interestingly, the sedative property of compound S5 was
negligible (5.09 %) when compared to chlorpheniramine
maleate (29.58 %).
Conclusion: Compound S5 can serve as a
lead molecule for further development into a new class
of H1-antihistaminic agents.
Keywords: Quinazolin-5-ones,
Antihistaminic activity, Histamine, Bronchoconstriction |
