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

被引：67

作者：

DeVita, RJ

Hollings, DD

Goulet, MT

Wyvratt, MJ

Fisher, MH

Lo, JL

Yang, YT

Cheng, K

Smith, RG

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(99)00446-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (similar to 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 1H-quinolone core. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2615 / 2620

页数：6

共 14 条

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