Preliminary Finding on a New Calcium Channel Entry Blocker Chemotype: 5,6-Diamino-4-hydroxy-2-mercaptopyrimidine Derivatives

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• 作者：Barbara Cosimelli ; Elda Severi ; Ettore Novellino ; Anna Cavaccini ; Mauro Cataldi ; Roberta Budriesi ; Matteo Micucci ; Alberto Chiarini ; Pierfranco Ioan
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：August 11, 2011
• 年：2011
• 卷：54
• 期：15
• 页码：5597-5601
• 全文大小：749K
• 年卷期：v.54,no.15(August 11, 2011)
• ISSN：1520-4804

文摘

We report the preliminary in vitro characterization of a series of pyrimidines as a new chemotype that modulates cardiovascular parameters and relaxes ileum smooth muscle according to classical calcium entry blockers. Tested compounds showed an interesting negative inotropic selectivity. In patch-clamp experiments they block L- over T-type calcium currents. Two requisites seem essential for the activity: lipophilic substituents in positions 2 and 5 of the pyrimidine ring and the acetamidic function in position 6.