Design, synthesis and primary activity of thiomorpholine derivatives as DPP-IV inhibitors |
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Authors: | Bei Han Jing Long Liu Yi Huan Peng Li Qi Wu Zi Yun Lin Zhu Fang Shen Da Li Yin Hai Hong Huang |
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Affiliation: | Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China |
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Abstract: | 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 4c, 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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Keywords: | Thiomorpholine Dipeptidyl peptidase IV inhibitor Synthesis Structure-activity relationship Oral glucose tolerance test |
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