Design and synthesis of novel 3-(4-Chlorophenyl)-2-(3-Substituted Propyl Thio) quinazolin-4-(3 H )-ones as a new class of H 1-antihistaminic Agents
Alagarsamy,V. 1Parthiban,P.1
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作者信息
1. Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy, Gr. Hyderabad-502 294
折叠
Abstract
A series of novel 3-(4-chlorophenyl)-2-(3-substituted propyl) quinazolin-4-(3H)-ones have been synthesized and tested for their in vivo H 1-antihistaminic activity on conscious guinea pigs. All the test compounds have protected the animals from histamine induced bronchospasm significantly. Compound 3-(4-chlorophenyl)-2-(3-(4-methylpiperazin-1-yl) propylthio) quinazolin-4(3H)-one (PC5) emerged as the most active compound (77.53% protection) of the series when compared to the reference standard chlorpheniramine maleate (70.09% protection). Compound PC5 shows negligible sedation (6.16%) compared to chlorpheniramine maleate (29.58%). Therefore, compound PC5 can serve as the lead molecule for further development into a new class of H 1-antihistaminic agents.
Key words
H 1-antihistaminic activity/quinazolin-4-ones/sedation
NSTL
Thieme Medical Publishers