Parallel and Mixture Combined Approach: Rapid Cheap Synthesis and Characterization of a 4096-Tripeptides Library

Autor: Gilles Subra, Jean-Louis Aubagnac, Jean Martinez, Christine Enjalbal, Laurent Soulère, Pascal Hoffmann
Rok vydání: 2003
Předmět:
Zdroj: QSAR & Combinatorial Science. 22:646-651
ISSN: 1611-020X
Popis: As part of a project that aims to discover novel inhibitors of the enzymes iron- superoxide dismutases (FeSODs), a library of 4096 N t e r -acetylated C t e r -amidated tripeptides was designed. To quickly and efficiently synthesize this library without any automation or expensive techniques, an original approach combining "sort and combine" and mixture syntheses was set up. For this purpose, rink amide Synphase Lanterns were chosen as pellicular solid support equipped with colour tagging systems. 512 discrete mixtures of eight tripeptides were prepared with only 64 Synphase D-Lanterns as starting materials. All the 512 mixtures were analyzed by ESI mass spectrometry Q-Tof in the positive mode showing that all the 4096 expected members of the library were present in comparable abundances with no trace of side-products. This paper demonstrates the usefulness of tagged and divisible Synphase lanterns allowing rapid and cheap generation of large organized discrete mixture libraries with high reliability.
Databáze: OpenAIRE