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Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.

Abstract：

:Sets of isomeric thiazole derivatives 1 and 2 have been synthesised in a parallel iterative solution-phase synthesis approach guided by the SAR analysis derived from biological results and computer-aided design and analysis. This synergistic and streamlined working procedure led to highly active isomeric NPY5 receptor ligands. However, a 10-fold difference at least in their respective binding affinities was consistently found for all isomeric pairs 1 and 2. The analysis of conformational differences due to heteroatom interactions in 1 and 2 revealed a favourable C=O...S interaction in 1, whereas thiazoles 2 showed a repulsive C=O...N interaction.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nettekoven M,Guba W,Neidhart W,Mattei P,Pflieger P,Roche O,Taylor S

doi

10.1016/j.bmcl.2005.05.009

subject

Has Abstract

pub_date

2005-07-15 00:00:00

pages

3446-9

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00562-7

journal_volume

15

pub_type

杂志文章

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