Hit to lead SAR study on benzoxazole derivatives for an NPY Y5 antagonist

被引：18

作者：

Omori, Naoki ^{[1
]}

Kouyama, Naoki ^{[1
]}

Yukimasa, Akira ^{[1
]}

Watanabe, Kana ^{[1
]}

Yokota, Yasunori ^{[1
]}

Tanioka, Hideki ^{[1
]}

Nambu, Hirohide ^{[1
]}

Yukioka, Hideo ^{[1
]}

Sato, Norihito ^{[2
]}

Tanaka, Yukari ^{[2
]}

Sekiguchi, Kazutaka ^{[2
]}

Okuno, Takayuki ^{[1
]}

机构：

[1] Shionogi & Co Ltd, Med Res Labs, Toyonaka, Osaka 5610825, Japan

[2] Shionogi & Co Ltd, Drug Dev Res Labs, Toyonaka, Osaka 5610825, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 05期

关键词：

Obesity; NPY Y5 receptor antagonist; GPCR; Benzoxazole; Hit to lead; RECEPTOR ANTAGONISTS; POTENT; DISCOVERY; DESIGN;

D O I：

10.1016/j.bmcl.2012.01.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report a hit to lead study on a novel benzoxazole NPY Y5 antagonist. Starting from HTS hit 1, structure-activity relationships were developed. Compound 12 showed reduction of food intake and a tendency to suppress body weight gain over the 21-day experimental period. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2020 / 2023

页数：4

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