title: 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.
abstract: 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 = 0.15 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.
authors: Universidad Nacional Autónoma de México, FES-Cuautitlán, Laboratorio de Química Medicinal, Campo 1. Av. 1ero de mayo S/N. 54714 Estado de México, México.
authors: Victor H
authors: VH
authors: Abrego
authors: Beatriz
authors: B
authors: Martínez-Pérez
authors: Luis A
authors: LA
authors: Torres
authors: Enrique
authors: E
authors: Angeles
authors: Luisa
authors: L
authors: Martínez
authors: J Lorena
authors: JL
authors: Marroquín-Pascual
authors: Rosario
authors: R
authors: Moya-Hernández
authors: Héctor Adrián
authors: HA
authors: Amaro-Recillas
authors: Juan Carlos
authors: JC
authors: Rueda-Jackson
authors: Damaris
authors: D
authors: Rodríguez-Barrientos
authors: Alberto
authors: A
authors: Rojas-Hernández
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000737:chemistry* / Q000494:pharmacology*; D000959:Antihypertensive Agents / Q000737:chemistry* / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D004095:Dihydropyridines / Q000737:chemistry* / Q000494:pharmacology*; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D009025:Morpholines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013056:Spectrophotometry, Ultraviolet
chemical_list: C554436:4-(4-hydroxy-3,5-bis(morpholin-4-ylmethyl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester; D000889:Anti-Arrhythmia Agents; D000959:Antihypertensive Agents; D004095:Dihydropyridines; D009025:Morpholines