A search for new antihypertensive agents. II. Circulatory activity and selection of structures among 2-methylbenzimidazole derivatives.
A series of twelve 2-methylbenzimidazole derivatives was prepared and their effect on the contraction of isolated rat tail artery, on beating rate and amplitude of isolated rat heart atria, on human blood platelet aggregation, and on blood pressure in urethane-anesthetized normotensive rats were tested. Numerical measures of pharmacodynamic activity were quantitatively related to the changes in chemical structure of the agents. Conclusions are drawn about the mechanism of pharmacodynamic action of 2-methylbenzimidazole derivatives, which is not executed directly through the adrenergic system. The further direction of synthesis is established basing on the results obtained.
Kaliszan
R
R
Biopharmaceutics and Pharmacodynamics Unit, Medical Academy, Gdańsk, Poland.
Foks
H
H
Damasiewicz
B
B
Nasal
A
A
Petrusewicz
J
J
Radwańska
A
A
Saczewski
F
F
Kuźmierkiewicz
W
W
D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006439:Hemodynamics / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D001562:Benzimidazoles