| Literature DB >> 24388688 |
Jean-Baptiste Veron1, Advait Joshi1, Charlotta Wallinder1, Mats Larhed1, Luke R Odell2.
Abstract
Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT2R ligand, were designed, synthesized and evaluated for their affinity to the AT2R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, Ki=8.5 μM) was over 12-times more potent than the lead compound 2.Entities:
Keywords: AT(1) receptor; AT(2) receptor; Angiotensin; Isoleucine
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Year: 2013 PMID： 24388688 DOI： 10.1016/j.bmcl.2013.12.040
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823