2. Academic Validation
  3. Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity

Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity

  • Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. doi: 10.1016/j.bmcl.2006.07.036.
Karsten Schnatbaum 1,  Elsa Locardi,  Dirk Scharn,  Uwe Richter,  Heiko Hawlisch,  Jochen Knolle,  Thomas Polakowski
Affiliations

Affiliation

  • 1 Jerini AG, Invalidenstrasse 130, 10115 Berlin, Germany. schnatbaum@jerini.de
PMID: 16876401 DOI: 10.1016/j.bmcl.2006.07.036
Abstract

A new class of peptidomimetic C5a receptor antagonists characterized by C-terminal Amino acids with hydrophobic side chains is presented. Systematic optimization of the first hits led to JPE1375 (36), which was intensively characterized in vitro and in vivo. Compound 36 exhibits high microsomal stability and receptor specificity and is highly active in an immune complex mediated peritonitis model (reverse passive Arthus reaction) in mice.

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