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

G Capozzi, S Giannini, S Menichetti, C Nativi…

文献索引：Capozzi, Giuseppe; Giannini, Sabrina; Menichetti, Stefano; Nativi, Cristina; Giolitti, Alessandro; Patacchini, Riccardo; Perrotta, Enzo; Altamura, Maria; Alberto Maggi, Carlo Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 17 p. 2263 - 2266

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被引用次数: 17

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.