Synthesis of a positional scanning library of pentamers of N-alkylglycines assisted by microwave activation and validation via the identification of trypsin inhibitors.
J Comb Chem
; 10(6): 974-80, 2008.
Article
de En
| MEDLINE
| ID: mdl-18847288
ABSTRACT
A positional scanning library of 625 N-alkylglycine pentamers has been synthesized on solid-phase, employing a set of 10 commercially available primary amines as a source of chemical diversity. The iterative synthetic steps were carried out in tea bags and accelerated by using microwave assisted organic synthesis (MAOS). The reactivity study of the primary amines used as diversity sources led to determine their relative reactivity values and equireactivity factors, which were applied to the library synthesis to ensure comparable concentrations of all final oligomers in the mixtures. This library was validated by the screening, deconvolution, and identification of trypsin inhibitors. These compounds are of potential interest for controlling the intracellular transport of TRPV1 channel.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Oligopeptides
/
Inhibiteurs trypsiques
/
Bibliothèques de petites molécules
/
Découverte de médicament
/
Glycine
Type d'étude:
Diagnostic_studies
/
Prognostic_studies
Langue:
En
Journal:
J Comb Chem
Sujet du journal:
QUIMICA
Année:
2008
Type de document:
Article
Pays d'affiliation:
Espagne