DARU Journal of Pharmaceutical Sciences 2004. 12(1):31-35.

"Assessment of human AT1 Binding Affinity of Some Novel 2-alkylthio-1-[4-(N-α-ethoxycarbonyl-nzyl)aminobenzyl-5-hydroxymethylimidazoles "
Setareh Badakhshannoory, Farhad.Hadizadeh, Abbas Shafiee


Antagonists of various components of the renin-angiotensin system have been the subject of many studies for the control of blood pressure. Compounds with a phenoxyphenylacetic acid moiety that mimic the structure of losartan which is a powerful competitive antagonist of angiotensin receptor, have shown to be effective. In this study, the affinity of some 2-alkylthio-1-[4-(N-α-ethoxycarbonylbenzyl)aminobenzyl]-5-hydroxymethyl imidazoles for the human AT1 receptor was assessed in a radioligand binding assay. It was found that an alkyl chain of appropriate length would be most suitable if situated on the imidazole ring. Furthermore, variations of the lower phenyl rings demonstrated that introduction of a methyl group in this position will account for the most desired effect.


Renin-angiotensin system, AngiotensinII, Losartan, Phenoxyphenylacetic acid, Radioligand binding assay,

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