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Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.

Abstract：

:A versatile parallel synthetic method to obtain three series of non-cyclic analogues of the first drug-like selective angiotensin II AT(2) receptor agonist (1) has been developed. In analogy with the transformation of losartan to valsartan it was demonstrated that a non-cyclic moiety could be employed as an imidazole replacement to obtain AT(2) selective compounds. In all the three series, AT(2) receptor ligands with affinities in the lower nanomolar range were found. None of the analogues exhibited any affinity for the AT(1) receptor. Four compounds, 17, 22, 39 and 51, were examined in a neurite outgrowth cell assay. All four compounds were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Murugaiah AM,Wallinder C,Mahalingam AK,Wu X,Wan Y,Plouffe B,Botros M,Karlén A,Hallberg M,Gallo-Payet N,Alterman M

doi

10.1016/j.bmc.2007.07.026

subject

Has Abstract

pub_date

2007-11-15 00:00:00

pages

7166-83

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(07)00613-X

journal_volume

15

pub_type

杂志文章

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