Quantitative relationships between hydrophobicity and hypotensive activity of diazacycloalkane derivatives.
The effect of a series of ten newly synthesized diazacycloalkanes as well as four standard imidazoline drugs on blood pressure of anesthetized normotensive rats was measured. The hypotensive activity of the agents studied, expressed as logit of the maximum effect, logit E(%), was quantitatively related to the changes in their chemical structure. Highly significant relationship between the hydrophobicity parameter, sigma f, and logit E(%) value has been found.
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Biopharmaceutics and Pharmacodynamics Unit, Medical Academy, Gdańsk, Poland.
Kaliszan
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Foks
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Wisterowicz
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K
D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002855:Chromatography, Thin Layer; D007093:Imidazoles / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D011719:Pyrazines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D007093:Imidazoles; D011719:Pyrazines