Glycosyl derivatives of NK2 tachykinin receptor antagonists

被引：7

作者：

Pinzani, D

Papini, AM

Vallecchi, ME

Chelli, M

Ginanneschi, M

Rapi, G

Quartara, L

Patacchini, R

Maggi, CA

Arcamone, FM

机构：

[1] UNIV FLORENCE,DIPARTIMENTO CHIM ORGAN UGO SCHIFF,I-50121 FLORENCE,ITALY

[2] UNIV FLORENCE,CTR CNR CHIM & STRUTTURA COMPOSTI ETEROCICLICI,I-50121 FLORENCE,ITALY

[3] A MENARINI IND FARMACEUT RIUNITE SR1,I-50131 FLORENCE,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 04期

关键词：

D O I：

10.1016/0960-894X(96)00039-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The influence of glycosylation on the structure-activity relationship of the tachykinin antagonist MEN 10376 and of its minimal active fragment MEN 10414 was investigated. The antagonist activity was preserved only when beta-D-glucosylated Tyr, Ser and Asn were added to the N-terminal position of MEN 10376, while the modification of the side chain of the Tyr(2) induced a dramatic decrease in affinity.

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页码：367 / 372

页数：6

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