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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.
- 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.)
- Subjects :
- Animals
Blood Pressure drug effects
Heart Rate drug effects
Male
Rats
Rats, Wistar
Spectrophotometry, Ultraviolet
Anti-Arrhythmia Agents chemistry
Anti-Arrhythmia Agents pharmacology
Antihypertensive Agents chemistry
Antihypertensive Agents pharmacology
Dihydropyridines chemistry
Dihydropyridines pharmacology
Morpholines chemistry
Morpholines pharmacology
Subjects
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