Discovery of Highly Polar β-homophenylalanine Derivatives as Non-systemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY(2019)
摘要
Although intensively expressed within intestine, the precise roles of intestinal dipeptidyl peptidase IV (DPPIV) in numerous pathologies remain incompletely understood. Here, we first reported a nonsystemic intestine-targeted (NSIT) DPPIV inhibitor with beta-homophenylalanine scaffold, compound 7, which selectively inhibited the intestinal rather than plasmatic DPPIV at an oral dosage as high as 30 mg/kg. We expect that compound 7 could serve as a qualified tissue selective tool to determine undetected physiological or pathological roles of intestinal DPPIV.
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关键词
dipeptidyl peptidase derivatives,inhibitors,intestine-targeted
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