Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor

被引：15

作者：

Capozzi, G

Giannini, S

Menichetti, S

Nativi, C

Giolitti, A

Patacchini, R

Perrotta, E

Altamura, M

Maggi, CA

机构：

[1] Univ Florence, Dipartimento Chim Organ Ugo Schiff, I-50019 Florence, Italy

[2] Univ Messina, Dipartimento Chim Organ & Biol, I-98166 Messina, Italy

[3] Menarini Ricerche SpA, I-50131 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00471-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Enantiopure cycloadducts between glycals and alkyl or aryl heterodienes were selected as small, rigid, nonpeptide molecules able to superimpose to the structure of the cyclopeptide tachykinin NK-2 antagonist 1. The presence of three aromatic groups in the pyranose ring resulted essential for NK-2 affinity, while an increase in activity was shown by the corresponding sulfoxides. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：2263 / 2266

页数：4

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