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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