THE DESIGN OF DIPEPTIDE HELICAL MIMETICS - THE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF TRISUBSTITUTED INDANES

Authors
HORWELL DC HOWSON W RATCLIFFE G WILLEMS H
Citation
Dc. Horwell et al., THE DESIGN OF DIPEPTIDE HELICAL MIMETICS - THE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF TRISUBSTITUTED INDANES, Bioorganic & medicinal chemistry letters, 4(24), 1994, pp. 2825-2830
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
24
Year of publication
1994
Pages
2825 - 2830
Database
ISI
SICI code
0960-894X(1994)4:24<2825:TDODHM>2.0.ZU;2-7
Abstract
The design and synthesis of conformationally constrained, non-peptide templates (trisubstituted indanes) which allow the incorporation of tw o adjacent amino acid side-chains plus a third binding group in an ori entation similar to that found in alpha-helices is reported. The tachy kinin receptor affinity of various Phe-Phe and Trp-Phe mimetics were d etermined and several were shown to bind with micromolar affinity.