Short pseudopeptides containing turn scaffolds with high AT2 receptor affinity
摘要:
Two pentapeptides, Ac-Tyr-Ile-His-Pro-Phe/Ile, were synthesized and shown to have angiotensin II AT(2) receptor affinity and agonistic activity. Based on these peptides, a new series of 13 pseudopeptides was synthesized via introduction of five different turn scaffolds replacing the Tyr-Ile amino acid residues. Pharmacological evaluation disclosed subnanomolar affinities for some of these compounds at the AT(2) receptor. Substitution of Phe by Ile in this series of ligands enhanced the AT(2) receptor affinity of all compounds. These results suggest that the C-terminal amino acid residues can be elaborated on to enhance the AT(2) receptor affinity in truncated Ang II analogues. (c) 2006 Elsevier Ltd. All rights reserved.
Short pseudopeptides containing turn scaffolds with high AT2 receptor affinity
摘要:
Two pentapeptides, Ac-Tyr-Ile-His-Pro-Phe/Ile, were synthesized and shown to have angiotensin II AT(2) receptor affinity and agonistic activity. Based on these peptides, a new series of 13 pseudopeptides was synthesized via introduction of five different turn scaffolds replacing the Tyr-Ile amino acid residues. Pharmacological evaluation disclosed subnanomolar affinities for some of these compounds at the AT(2) receptor. Substitution of Phe by Ile in this series of ligands enhanced the AT(2) receptor affinity of all compounds. These results suggest that the C-terminal amino acid residues can be elaborated on to enhance the AT(2) receptor affinity in truncated Ang II analogues. (c) 2006 Elsevier Ltd. All rights reserved.
Quinoline derivatives as antagonists of leukotriene D.sub.4
申请人:Rhone-Poulenc Rorer Pharmaceuticals Inc.
公开号:US05051427A1
公开(公告)日:1991-09-24
This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.
Quinoline derivatives and use thereof as antagonists of leukotriene D.sub.4
申请人:Rorer Pharmaceutical Corp.
公开号:US04920133A1
公开(公告)日:1990-04-24
This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.