2. Academic Validation
  3. Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands

Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands

  • ACS Med Chem Lett. 2014 Dec 8;6(2):178-82. doi: 10.1021/ml500427r.
Charlotta Wallinder 1,  Christian Sköld 1,  Milad Botros 2,  Marie-Odile Guimond 3,  Mathias Hallberg 2,  Nicole Gallo-Payet 3,  Anders Karlén 1,  Mathias Alterman 1
Affiliations

Affiliations

  • 1 Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, BMC, Uppsala University , SE-751 23 Uppsala, Sweden.
  • 2 Beijer Laboratory, Department of Pharmaceutical Biosciences, BMC, Uppsala University SE-751 23 Uppsala, Sweden.
  • 3 Service of Endocrinology, Faculty of Medicine and Heath Sciences, University of Sherbrooke , Sherbrooke J1H 5N4, Quebec, Canada.
PMID: 25699147 DOI: 10.1021/ml500427r
Abstract

Migration of the methylene imidazole side chain in the first reported selective drug-like AT2 Receptor Agonist C21/M024 (1) delivered the AT2 Receptor Antagonist C38/M132 (2). We now report that the AT2 Receptor Antagonist compound 4, a biphenyl derivative that is structurally related to 2, is transformed to the agonist 6 by migration of the isobutyl group. The importance of the relative position of the methylene imidazole and the isobutyl substituent is highlighted herein.

Keywords

AT2 receptor; C21/M024; C38/M132; agonist; antagonist; nonpeptide ligands.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z