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

Naoki Omori,Naoki Kouyama,Akira Yukimasa,Kana Watanabe,Yasunori Yokota,Hideki Tanioka,Hirohide Nambu,Hideo Yukioka,Norihito Sato,Yukari Tanaka,Kazutaka Sekiguchi,Takayuki Okuno

Bioorganic & Medicinal Chemistry Letters（2012）

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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.

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关键词

Obesity,NPY Y5 receptor antagonist,GPCR,Benzoxazole,Hit to lead

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