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2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.

Abstract：

:This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wyatt PG,Allen MJ,Borthwick AD,Davies DE,Exall AM,Hatley RJ,Irving WR,Livermore DG,Miller ND,Nerozzi F,Sollis SL,Szardenings AK

doi

10.1016/j.bmcl.2005.03.045

subject

Has Abstract

pub_date

2005-05-16 00:00:00

pages

2579-82

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00350-1

journal_volume

15

pub_type

杂志文章

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