Synthesis and antagonistic activity of four new 2-alkyl-N-biphenyl fused imidazoles on angiotensin II receptors.
In the current study, four new 2-alkyl-N-biphenyl fused imidazoles were synthesized and the pharmacological properties of these compounds as angiotensin II antagonists were studied. First, the potency of the synthesized compounds on guinea-pig ileum was evaluated and the vasopressor effect of the most potent compound 6a was compared with losartan on isolated perfused rat kidney. The antagonistic activity of compound 6a (sodium 2-propyl-5-carbomethoxy-1-[(biphenyl-4-yl)methyl]pyrrolo[3,2-d]imidazole-2'-carboxylate) on angiotensin II receptors was greater than the other synthesized compounds and in isolated perfused rat kidney was similar to losartan.
Razi Institute for Drug Research, Iran University of Medical Sciences, Shaheed Hemmat Expressway, Tehran, Iran.
Maziar M
MM
Akhavan
Javid Shahbazi
JS
Mojarrad
Ali
A
Rouzrokh
Sultan A
SA
Ebrahimi
Massoud
M
Mahmoudian
Abbas
A
Shafiee
D000804:Angiotensin II / Q000494:pharmacology; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D011945:Receptors, Angiotensin / Q000502:physiology; D014661:Vasoconstriction / Q000187:drug effects / Q000502:physiology
D057911:Angiotensin Receptor Antagonists; D007093:Imidazoles; D011945:Receptors, Angiotensin; D000804:Angiotensin II