GLYCOSYL DERIVATIVES OF NK2 TACHYKININ RECEPTOR ANTAGONISTS

Authors
PINZANI D PAPINI AM VALLECCHI ME CHELLI M GINANNESCHI M RAPI G QUARTARA L PATACCHINI R MAGGI CA ARCAMONE FM
Citation
D. Pinzani et al., GLYCOSYL DERIVATIVES OF NK2 TACHYKININ RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(4), 1996, pp. 367-372
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
4
Year of publication
1996
Pages
367 - 372
Database
ISI
SICI code
0960-894X(1996)6:4<367:GDONTR>2.0.ZU;2-5
Abstract
The influence of glycosylation on the structure-activity relationship of the tachykinin antagonist MEN 10376 and of its minimal active fragm ent MEN 10414 was investigated. The antagonist activity was preserved only when beta-D-glucosylated Tyr, Ser and Asn were added to the N-ter minal position of MEN 10376, while the modification of the side chain of the Tyr(2) induced a dramatic decrease in affinity.