Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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The Cardiovascular Properties of Some Amide Derivatives of Pyrimidin-8-on[2,1-f]theophylline-9- Alkylcarboxylic Acids

Author(s): A. Zagorska, O. Fhid, M. Pawlowski, B. Filipek, M. Zygmunt.

Abstract:

N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamides of pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids were prepared and preliminary tested for their cardiovascular activity. Some of the tested compounds presented effects on arrhythmia parameters and blood pressure. The most interesting were dialkylamino-alkylamides and their morpholine analogs (4a-10a), which protected the heart against the bradycardia and diminished mortality of animals. In comparison to the chinidini sulfas the strongest activity was observed for diethylaminoethylamide of pyrimidin-8-on[2,1- f]theophylline-9-acetic acid (4a). Amides (1-3) without the basic center in the substituent showed weak antihypertensive properties.

Keywords: Antiarrhythmic agents, adenosine receptors antagonists, pyrimido[2,1-f-]theophylline-9-alkylcarboxylic acids amides, cardiovascular activity of fused [2,1-f]theophyllines, tricyclic theophylline derivatives

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Article Details

VOLUME: 3
ISSUE: 5
Year: 2006
Page: [346 - 350]
Pages: 5
DOI: 10.2174/157018006777574159
Price: $58