Premium
An Efficient Combinatorial Method for the Discovery of Glycosidase Inhibitors
Author(s) -
GerberLemaire Sandrine,
Popowycz Florence,
RodríguezGarcía Eliazar,
Asenjo Ana Teresa Carmona,
Robina Inmaculada,
Vogel Pierre
Publication year - 2002
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/1439-7633(20020503)3:5<466::aid-cbic466>3.0.co;2-d
Subject(s) - imine , drug discovery , combinatorial chemistry , computer science , glycoside hydrolase , computational biology , chemistry , work (physics) , stereochemistry , biochemistry , enzyme , biology , engineering , catalysis , mechanical engineering
A dynamic imine library formed in solution provides a fast route to drug discovery. Imine formation from diamine 4 and a sublibrary of aldehydes can be used for the efficient discovery of glycosidase inhibitors through a new combinatorial approach. When the equilibrium shown is reached rapidly under dilute conditions, a mixture of imines is produced and can be screened by the glycosidase, which binds preferentially to the best inhibitor.