Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases

…, S Scharpé, A Haemers, K Augustyns

文献索引：Van Der Veken, Pieter; Senten, Kristel; Kertesz, Istvan; De Meester, Ingrid; Lambeir, Anne-Marie; Maes, Marie-Berthe; Scharpe, Simon; Haemers, Achiel; Augustyns, Koen Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1768 - 1780

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被引用次数: 80

摘要

The feasibility of the fluoro-olefin function as a peptidomimetic group in inhibitors for dipeptidyl peptidase IV and II (DPP IV and DPP II) is investigated by evaluation of N- substituted Gly-Ψ [CF C] pyrrolidines, Gly-Ψ [CF C] piperidines, and Gly-Ψ [CF C](2-cyano) pyrrolidines. Of this later class, the (Z)-and (E)-fluoro-olefin analogues were prepared and chemical stability in comparison with the parent amide was checked. Most of these ...