Title of article :
Highly Efficient, One Pot, Solvent and Catalyst, Free Synthesis of Novel Quinazoline Derivatives under Ultrasonic Irradiation and Their Vasorelaxant Activity Isolated Thoracic Aorta of Rat
Author/Authors :
Purkhosrow, Azar Department of Pharmacology - School of Medicine - Shiraz University of Medical Sciences, Shiraz, Iran , Khalili, Azadeh Department of Physiology and Pharmacology - School of Medicine - Alborz University of Medical Sciences, Karaj, Iran , Chih Ho, Anthony Department of Chemistry and Biochemistry - School of Science - University of Arizona, Tucson, Arizona, United States , Mowlazadeh Haghighi, Saghar Department of Chemistry - School of Science - Shiraz University of Science, Shiraz, Iran , Fakher, Shima Department of Pharmacology - School of Medicine - Shiraz University of Medical Sciences, Shiraz, Iran , Khalafi Nezhad, Ali Department of Chemistry - School of Science - Shiraz University of Science, Shiraz, Iran
Abstract :
New quinazoline derivatives were prepared by one pot reaction of anthranilic acid, acetic
anhydride and primary amines, under ultrasonic irradiation. As a result, Ultrasonic irradiation
has led to affordable, clean synthesis of a variety of target compounds in much higher yields,
than traditional methods. This method has numerous advantages: such as higher yields,
shorter reactions time, and easier work-up. Several structural classes among these compounds
were identified to have vasorelaxant activity. In this respect, all of the newly synthesized
quinazolinone derivatives displayed vasorelaxant properties on the isolated thoracic rat aorta.
The IC50 of compounds 2a (-6.00 ± 0.55), 2g (-7.31 ± 0.94), 2n (-7.15 ± 0.81) and 2p (-7.77
± 0.31) was comparable to that seen in the Acetylcholine (-7.13 ± 0.14). The structures of
the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectral
studies, elemental analysis, and melting point.
Keywords :
One pot , Thoracic aorta of rat , Vasorelaxant activity , Ultrasonic irradiation , Quinazoline
Journal title :
Astroparticle Physics