title: Synthesis of thioether derivatives of quinazoline-4-one-2-thione and evaluation of their antiplatelet aggregation activity.
abstract: A series of 2-(arylmethylthio)-3-phenylquinazolin-4-one derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma. Among the tested thioethers, derivative 2, 3, 5 and 16 were the most potent compounds with satisfactory IC50 for inhibition of platelet aggregation induced by ADP. Analysis of global physicochemical parameters shows some correlations between activities and molecular volume and also surface area of the studied derivatives.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Vali Asr Avenue, Niayesh Junction, P.O. Box 14155-6153, Tehran, Iran.
authors.forename: Zahra
authors.initials: Z
authors.lastname: Eskandariyan
authors.forename: Marjan
authors.initials: M
authors.lastname: Esfahani Zadeh
authors.forename: Kamaleddin
authors.initials: K
authors.lastname: Haj Mohammad Ebrahim Tehrani
authors.forename: Vida
authors.initials: V
authors.lastname: Mashayekhi
authors.forename: Farzad
authors.initials: F
authors.lastname: Kobarfard
mesh_terms: D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects* / Q000502:physiology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013440:Sulfides / Q000138:chemical synthesis* / Q000494:pharmacology; D013871:Thiones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D010975:Platelet Aggregation Inhibitors; D011799:Quinazolines; D013440:Sulfides; D013871:Thiones