cardiovascular-agents and imidazole

A series of novel substituted imidazole derivatives were synthesized and have been screened in vivo for their hypotensive and acute toxicity activities. Out of seventeen compounds eight compounds (2b, 2c, 3b, 3c, 3f, 4a, 4b and 4c) have shown good hypotensive and bradycardiac responses. Compounds 3b, 3c, 3f and 4c have shown better activity than reference drug clonidine. All the compounds have shown ALD50>1000 mg/kg with maximum in 2e and 4c (>1200 mg/kg).

Topics: Animals; Blood Pressure; Cardiovascular Agents; Cats; Heart Rate; Imidazoles; Structure-Activity Relationship

Pretreatment of rats by the cyclooxygenase inhibitors diclofenac, phenylbutazone, and aminophenazone did not influence kappa-carrageenin (KC) rat tail thrombosis (RTT) whereas pretreatment by aspirin, at high doses, and particularly sulfinpyrazone decreased RTT frequency, PGI2 or iloprost i.v. injection showed strong RTT preventing effects as it was also seen by thromboxane synthesis inhibitors (benzydamine, imidazole) at high doses. The PAF antagonist BN 52020 weakly protected. Lipoxygenase inhibitors (quercetin, oxphaman a.o.) proved ineffective. Therefore, thromboxane/PGI2 balance and partly PAF seem to be involved in the mechanism of KC RTT.

Topics: Aminopyrine; Animals; Aspirin; Benzydamine; Cardiovascular Agents; Carrageenan; Diclofenac; Epoprostenol; Female; Iloprost; Imidazoles; Phenylbutazone; Rats; Rats, Inbred Strains; Thrombosis; Thromboxanes; Trapidil