title: Preliminary finding on a new calcium channel entry blocker chemotype: 5,6-diamino-4-hydroxy-2-mercaptopyrimidine derivatives.
abstract: 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.
authors.affiliation: Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli Federico II, Napoli, Italy. barbara.cosimelli@unina.it
authors.forename: Barbara
authors.initials: B
authors.lastname: Cosimelli
authors.forename: Elda
authors.initials: E
authors.lastname: Severi
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Anna
authors.initials: A
authors.lastname: Cavaccini
authors.forename: Mauro
authors.initials: M
authors.lastname: Cataldi
authors.forename: Roberta
authors.initials: R
authors.lastname: Budriesi
authors.forename: Matteo
authors.initials: M
authors.lastname: Micucci
authors.forename: Alberto
authors.initials: A
authors.lastname: Chiarini
authors.forename: Pierfranco
authors.initials: P
authors.lastname: Ioan
mesh_terms: D000631:Aminopyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020746:Calcium Channels, L-Type / Q000187:drug effects; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D018408:Patch-Clamp Techniques; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000494:pharmacology
chemical_list: D000631:Aminopyridines; D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; D011743:Pyrimidines; D014665:Vasodilator Agents; C064001:pyrimidine-2-thiol