Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group

…, S Takai, A Kinoshita, A Hatayama, S Yamamoto…

文献索引：Kondo, Takashi; Nekado, Takahiro; Sugimoto, Isamu; Ochi, Kenya; Takai, Shigeyuki; Kinoshita, Atsushi; Hatayama, Akira; Yamamoto, Susumu; Kishikawa, Katsuya; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 4 p. 1613 - 1631

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被引用次数: 24

摘要

A series of (4β-substituted)-l-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of a N-(3-phenyl-1, 2, 4- thiadiazol-5-yl) piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound 26 ...