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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.

Authors :
Abrego VH
Martínez-Pérez B
Torres LA
Angeles E
Martínez L
Marroquín-Pascual JL
Moya-Hernández R
Amaro-Recillas HA
Rueda-Jackson JC
Rodríguez-Barrientos D
Rojas-Hernández A
Source :
European journal of medicinal chemistry [Eur J Med Chem] 2010 Oct; Vol. 45 (10), pp. 4622-30. Date of Electronic Publication: 2010 Jul 23.
Publication Year :
2010

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.<br /> (Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.)

Details

Language :
English
ISSN :
1768-3254
Volume :
45
Issue :
10
Database :
MEDLINE
Journal :
European journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
20705371
Full Text :
https://doi.org/10.1016/j.ejmech.2010.07.027