Synthesis and antihypertensive activity of novel 3 -benzyl -2 -substituted -3H-[1,2,4 ]triazolo[5,1-b]quinazolin -9 -ones

A series of 3-benzyl-2-substituted-3H-[1,2,4]triazolo[5,1-b]quinazolin-9-ones have been synthesized by the cyclocondensation of 3-amino-2-benzylamino-3H-quinazolin-4-one with a variety of one-carbon donors. The starting material 3-amino-2-benzylamino-3H-quinazolin-4-one was synthesized from methyl a...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2007-05, Vol.15 (10), p.3457-3462
Main Authors: ALAGARSAMY, Veerachamy, PATHAK, Urvishbhai S
Format: Article
Language:English
Subjects:
Animals
Antihypertensive agents
Antihypertensive Agents - chemical synthesis
Antihypertensive Agents - pharmacology
Biological and medical sciences
Blood Pressure - drug effects
Cardiovascular system
Indicators and Reagents
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Pharmacology. Drug treatments
Quinazolinones - chemical synthesis
Quinazolinones - pharmacology
Rats
Rats, Inbred SHR
Spectrophotometry, Infrared
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of 3-benzyl-2-substituted-3H-[1,2,4]triazolo[5,1-b]quinazolin-9-ones have been synthesized by the cyclocondensation of 3-amino-2-benzylamino-3H-quinazolin-4-one with a variety of one-carbon donors. The starting material 3-amino-2-benzylamino-3H-quinazolin-4-one was synthesized from methyl anthranilate by a novel innovative route. The title compounds were evaluated for their in vivo antihypertensive activity using spontaneously hypertensive rats (SHR). While all the test compounds exhibited significant antihypertensive activity, 3-benzyl-2-methyl-3H-[1,2,4]triazolo[5,1-b] quinazolin-9-one exhibited antihypertensive activity more than the reference standard prazocin.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2007.03.007