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Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics

Authors:	Naoki Taka Hiroharu Matsuoka Tsutomu Sato Hitoshi Yoshino Ikuhiro Imaoka Haruhiko Sato Ken-ichiro Kotake Yoshikazu Kumagai Kenshi Kamei Ken-ichi Ozaki Atsuko Higashida Toshio Kuroki

Institution:	1. Chemistry Research Dept. 1, Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan;2. Pharmaceutical Technology Dept., Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan;3. CMC Planning and Coordination Dept., Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan;4. Pharmaceutical Research Dept. 1, Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan;5. Discovery Platform Technology Dept., Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan;6. Research Planning and Coordination Dept., Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado Gotemba City, Shizuoka 412-8513, Japan

Abstract:	We successfully discovered peptidomimetic motilin antagonists (17c and 17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.

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