Abstract
The concentration-response curves were constructed for 18 azole derivatives (including seven imidazoline drugs) as the inhibitors of the adrenaline-induced human blood platelet aggregation. It was demonstrated by the quantitative structure-activity relationships analysis that the less hydrophobic agents started to act as effective inhibitors at lower concentrations but that stronger effects could be obtained with the more hydrophobic derivatives. The conclusion was drawn that the inhibitory activity observed was the result of nonspecific hydrophobic interactions of the agents with both an andrenergic platelet receptor and a site of loss on serum albumin.
This is a preview of subscription content, log in via an institution to check access.
References
J. Petrusewicz and R. Kaliszan,Effect of imidazoline drugs on human blood platelet aggregation, Thromb. Haemostasis54, 784–787 (1985).
J. Petrusewicz and R. Kaliszan,Blood platelet adrenoceptor: Aggregatory and antiaggregatory activity of imidazoline drugs, Pharmacology33, 249–255 (1986).
R. Kaliszan, H. Foks, B. Damasiewicz, A. Nasal, A. Radwańska, W. Kuźmierkiewicz, D. Pancechowska-Ksepko, W. Rudnicka and K. Wisterowicz,A search for new antihypertensive agents. I. Alpha-adrenergic activity and selection of structures among pyrazine substituted imidazolines, Pol. J. Pharmacol. Pharm.37, 85–93 (1985).
R. Kaliszan, B. Damasiewicz, A. Nasal, A. Radwańska, H. Foks, W. Kuźmierkiewicz, D. Pancechowska-Ksepko, W. Rudnicka, K. Wisterowicz and K. Ośmiałowski,Structure and alpha-adrenergic activity of pyrazinimidazolines, Agents and Actions16, 435–442 (1985).
G. V. R. Born,Aggregation of blood platelets by adenosine diphosphate and its reversal, Nature194, 927–929 (1962).
C. Hanch and A. Leo,Substituent Constants for Correlation Analysis in Chemistry and Biology, Wiley-Interscience, New York 1979.
R. Kaliszan,Quantitative relationships between molecular structure and chromatographic retention. Implications in physical, analytical, and medicinal chemistry, CRC Crit. Rev. Anal. Chem.16, 323–383 (1986).
R. Jankowski, R. Kaliszan and H. Lamparczyk,Computer program for studies of quantitative structure-biological activity relationships by the Hansch method (in Polish), Acta Polon. Pharm.37, 573–577 (1980).
C. Hansch and A. Steward,The use of substituents constants in the analysis of the structure-activity relationships in penicillin derivatives. J. Med. Chem.7, 691–916 (1964).
A. Leo,Parameter and structure-activity data bases: Management for maximum utility, Environ. Health Perspect.61, 275–285 (1985).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Petrusewicz, J., Kaliszan, R. Antiaggregatory activity of imidazoline drugs and chemicals as a function of their structure. Agents and Actions 24, 204–209 (1988). https://doi.org/10.1007/BF01968102
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF01968102