Volume 28, Issue 20
Natural Products
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ChemInform Abstract: 2,3-Substituted 2-Azanorbornanes as Polar β-Turn Mimetics.

D. C. HORWELL

D. C. HORWELL

Parke-Davis Neurosci. Res. Cent., Cambridge Univ. Forvie Site, Cambridge CB2 2QB, UK

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D. NAYLOR

D. NAYLOR

Parke-Davis Neurosci. Res. Cent., Cambridge Univ. Forvie Site, Cambridge CB2 2QB, UK

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H. M. G. WILLEMS

H. M. G. WILLEMS

Parke-Davis Neurosci. Res. Cent., Cambridge Univ. Forvie Site, Cambridge CB2 2QB, UK

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First published: 04 August 2010

Abstract

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ChemInform Abstract

The conformationally restrained Trp-Phe mimetic (X) is constructed which is designed to mimic the size and direction of the dipole moment as well as the orientation of the two central amino acid side chains in a β-turn. The tachykinin receptor affinities of (X) are evaluated and compared to those of the NK-2 antagonist MEN 10627.

chemical structure image

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