【摘 要】
：
Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase Ⅳ (DPP-Ⅳ) inhibitors,with natural and non-natural L-amino acid
【机 构】
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Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation
【基金项目】
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We thank the Fundamental Scientific Research Fund of Institute of Materia Medica (Li Peng 504-Basic 10 DPP Ⅳ inhibitor) for financial support on this project
论文部分内容阅读
Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase Ⅳ (DPP-Ⅳ) inhibitors,with natural and non-natural L-amino acids as the starting materials.Their structures were characterized by 1H NMR,13C NMR and HR-MS.The target compounds were screened for the DPP-Ⅳ inhibition,and the preliminary SAR result was obtained.Particularly,compounds 4e,4d and 4f with good DPP-Ⅳ inhibition in vitro were further evaluated through a mouse oral glucose tolerance test (OGTT).The preliminary result showed the potential value for further studies on those thiomorpholine-bearing compounds as DPP-Ⅳ inhibitors.
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