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.
Cosimelli B, Severi E, Novellino E, Cavaccini A, Cataldi M, Budriesi R, et al. (2011). Preliminary Finding on a New Calcium Channel Entry Blocker Chemotype: 5,6-Diamino-4-hydroxy-2-mercaptopyrimidine Derivatives. JOURNAL OF MEDICINAL CHEMISTRY, 54, 5597-5601 [10.1021/jm200414s].
Preliminary Finding on a New Calcium Channel Entry Blocker Chemotype: 5,6-Diamino-4-hydroxy-2-mercaptopyrimidine Derivatives.
BUDRIESI, ROBERTA;MICUCCI, MATTEO;CHIARINI, ALBERTO;IOAN, PIERFRANCO
2011
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
