title: Design and synthesis of novel 3-(4-chlorophenyl)-2-(3-substituted propyl thio) quinazolin-4-(3H)-ones as a new class of H1-antihistaminic agents.
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 H1-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 H1-antihistaminic agents.
authors.affiliation: Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy, Hyderabad, Andhra Pradesh, India. drvalagarsamy@gmail.com
authors.forename: V
authors.initials: V
authors.lastname: Alagarsamy
authors.forename: P
authors.initials: P
authors.lastname: Parthiban
mesh_terms: D000818:Animals; D001986:Bronchial Spasm / Q000139:chemically induced / Q000517:prevention & control; D002744:Chlorpheniramine / Q000494:pharmacology; D006168:Guinea Pigs; D006632:Histamine / Q000008:administration & dosage; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D008297:Male; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D006634:Histamine H1 Antagonists; D052999:Quinazolinones; D002744:Chlorpheniramine; D006632:Histamine