Antihypertensive and antiarrhythmic properties of a para-hydroxy[bis(ortho-morpholinylmethyl)]phenyl-1,4-DHP compound: Comparison with other compounds of the same kind and relationship with logP values

作者：Abrego Victor H; Martinez Perez Beatriz; Torres Luis A; Angeles Enrique; Martinez Luisa; Lorena Marroquin Pascual J; Moya Hernandez Rosario; Adrian Amaro Recillas Hector; Carlos Rueda Jackson Juan; Rodriguez Barrientos Damaris; Rojas Hernandez Alberto

来源：European Journal of Medicinal Chemistry, 2010, 45(10): 4622-4630.

DOI：10.1016/j.ejmech.2010.07.027

• Cardiovascular effects
• Antihypertensives
• Bis(morpholinylmethyl)phenols
• DHP
• pKa values
• logP

A new para-hydroxy[bis(ortho-morpholinylmethyl)]phenyl-1,4-DHP substituted compound, (4-(4-hydroxy-3,5-bis(morpholin-4-ylmethyl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester. LQM300), with antihypertensive and antiarrhythmic properties, has been synthesized. Four pKa values of this compound have been determined with the aid of the program SQUAD, at pseudo-physiological conditions (T = 37 degrees C and I = 015 M) by UV spectrophotometry and at T = 25 degrees C and I = 0.05 M by Capillary Zone Electrophoresis (CZE). The logP = 2.7 +/- 0.2 between n-octanol and water, has been estimated by UV spectrophotometry. The antihypertensive and antiarrhythmic efficacies as well as the logP values have been compared with other compounds of the same kind and related with their structure.

• 出版日期2010-10