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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists.
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Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists.

机译:具有沙利度胺相关的α-葡萄糖苷酶抑制剂和肝X受体拮抗剂衍生的具有苯乙基苯基邻苯二甲酰亚胺骨架的非竞争性和选择性二肽基肽酶IV抑制剂。

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摘要

Novel dipeptidyl peptidase IV (DPP-IV) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on alpha-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Representative compounds showed non-competitive inhibition of DPP-IV and 28a exhibited 10-fold selectivity for DPP-IV over DPP-8. Compound 28a is the first non-competitive, selective DPP-IV inhibitor.
机译:基于α-葡萄糖苷酶抑制剂和沙利度胺衍生的肝X受体(LXR)拮抗剂,制备了具有苯乙基苯基邻苯二甲酰亚胺骨架的新型二肽基肽酶IV(DPP-IV)抑制剂。代表性化合物显示出对DPP-IV的非竞争性抑制作用,并且28a对DPP-IV的选择性是DPP-8的10倍。化合物28a是第一种非竞争性选择性DPP-IV抑制剂。

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