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Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.

Abstract：

:A new class of kappa-opioid receptor agonists is described. The design of these agents was based upon energy minimization and structural overlay studies of the generic azepin-2-one structure 3 with the crystal structure of arylacetamide kappa agonist 1, ICI 199441. The most active compound identified was ligand 4a (K(i)=0.34 nM), which demonstrated potent antinociceptive activity after oral administration in rodents.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tuthill PA,Seida PR,Barker W,Cassel JA,Belanger S,DeHaven RN,Koblish M,Gottshall SL,Little PJ,DeHaven-Hudkins DL,Dolle RE

doi

10.1016/j.bmcl.2004.08.041

subject

Has Abstract

pub_date

2004-11-15 00:00:00

pages

5693-7

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01049-2

journal_volume

14

pub_type

杂志文章

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