Non-peptide peptidomimetics and related cyclic hexapeptides
申请人:The Trustees of the University of Pennsylvania
公开号:US05811512A1
公开(公告)日:1998-09-22
Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor.
提供的化合物与那些结合G蛋白偶联受体的肽具有交叉反应性,以及用于这些化合物的制备和治疗方法。
Non-Peptide peptidomimetics
申请人:The Trustees of the University of Pennsylvania
公开号:US05552534A1
公开(公告)日:1996-09-03
Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 comprises a functional group which is chemically similar to that found in the peptide of interest.
申请人:The Trustees of the University of Pennsylvania
公开号:US06197963B1
公开(公告)日:2001-03-06
Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure:
wherein at least one of R1, R2, R3, R4, or R5 comprises a functional group which is chemically similar to that found in the peptide of interest.
Chemoselective monoalkylation of 5-trifluoroacetamido- and 5-acetamido-1-pentanol derivatives via N,O-bisdeprotonation. Quantitation of evolved H2 as a probe of anion formation
作者:Ralph Hirschmann、John Hynes、P.Grant Spoors、Amos B. Smith
DOI:10.1016/0040-4039(95)00280-p
日期:1995.4
Measurements of H-2 evolution revealed that neither 5-trifluoroacetamido-1-pentanol (1) nor 5-acetamido-1-pentanol (6) underwent complete bisdeprotonation upon treatment with excess NaH in THF, thereby accounting for the unexpected course of subsequent alkylations with carbohydrate-derived triflates 2 and 7. These studies in turn led to an effective protocol for generation of N,O-dianions from 1 and 6; as anticipated, the former chemoselectively furnished O-alkylation products with triflates 2 and 15.