Potential antihypertensive benzimidazole derivatives.
A series of benzimidazole derivatives was synthesized and tested for their hypotensive activity. The most interesting compounds were: BS1/81 (2-guanidino-benzimidazole) and BS1/84 (2-guanidino-5-aminobenzimidazole dihydrochloride), which effects were comparable to those of aminophylline. It was found that substitution of guanidine nitrogen atom with phenyl group caused a distinct decrease of activity while cyclization of guanidine rest to pyrimidine ring caused only a small decrease of activity.
Serafin
B
B
Institute of Organic Technology, Technical University (Politechnika), Warszaw, Poland.
Borkowska
G
G
Główczyk
J
J
Kowalska
I
I
Rump
S
S
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001794:Blood Pressure / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D004562:Electrocardiography; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains
D000889:Anti-Arrhythmia Agents; D000959:Antihypertensive Agents; D001562:Benzimidazoles