Investigation of SAR requirements of SR 142801 through an indexed combinatorial library in solution

Authors
Raveglia, LF Vitali, M Artico, M Graziani, D Hay, DWP Luttmann, MA Mena, R Pifferi, G Giardina, GAM
Citation
Lf. Raveglia et al., Investigation of SAR requirements of SR 142801 through an indexed combinatorial library in solution, EUR J MED C, 34(10), 1999, pp. 825-835
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
02235234 → ACNP
Volume
34
Issue
10
Year of publication
1999
Pages
825 - 835
Database
ISI
SICI code
0223-5234(199910)34:10<825:IOSROS>2.0.ZU;2-3
Abstract
To rapidly gain information on structure-activity relationship (SAR) requir ements of the human neurokinin 3 (hNK-3) receptor antagonist SR 142801, an indexed combinatorial Library was synthesised in solution and screened on t he hNK-3 receptor. SAR considerations drawn from binding affinity of combin atorial mixtures were confirmed through the synthesis and biological evalua tion of some individual compounds. (C) 1999 Editions scientifiques et medic ales Elsevier SAS.