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Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.

Abstract：

:Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (approximately 300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chloro-substitution of the 1 H-quinolone core.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

DeVita RJ,Hollings DD,Goulet MT,Wyvratt MJ,Fisher MH,Lo JL,Yang YT,Cheng K,Smith RG

doi

10.1016/s0960-894x(99)00446-1

subject

Has Abstract

pub_date

1999-09-06 00:00:00

pages

2615-20

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X99004461

journal_volume

9

pub_type

杂志文章

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