Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
Methods and compositions for ribosomal synthesis of macrocyclic peptides
申请人:University of Rochester
公开号:US10544191B2
公开(公告)日:2020-01-28
Methods and compositions are provided for generating macrocyclic peptides from genetically encoded, ribosomally produced polypeptide precursors. Also provided are nucleic acid molecules, polypeptides, and methods for generating combinatorial libraries of macrocyclic peptides. These methods can be used to produce vast libraries of conformationally constrained peptide ligands as well as facilitate the functional screening of these libraries to identify compound(s) with desired activity properties.
[EN] METHODS AND COMPOSITIONS FOR RIBOSOMAL SYNTHESIS OF MACROCYCLIC PEPTIDES<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR LA SYNTHÈSE RIBOSOMIQUE DE PEPTIDES MACROCYCLIQUES
申请人:UNIV ROCHESTER
公开号:WO2015100277A9
公开(公告)日:2015-10-01
Identification of potent phenyl imidazoles as opioid receptor agonists
作者:Henry J. Breslin、Chaozhong Cai、Tamara A. Miskowski、Santosh V. Coutinho、Sui-Po Zhang、Pamela Hornby、Wei He
DOI:10.1016/j.bmcl.2006.01.082
日期:2006.5
Using previously reported opioid receptor (OR) agonist analogs 4a-c as starting points, the structure-activity relationship (SAR) for their related series has been further refined. This SAR Study has led to the identification of 2,6-di-Me-Tyr (DMT) analogs 4h and 4j as the most potent OR agonist within the series. in addition, it was discovered that 4-(aminocarbonyl)-2,6-dimethyl-Phe is a reasonable bioisostere surrogate for the DMT moiety, as supported by the OR activities Of Compounds 4x and 4y. (C) 2006 Elsevier Ltd. All rights reserved.
METHODS AND COMPOSITIONS FOR RIBOSOMAL SYNTHESIS OF MACROCYCLIC PEPTIDES