Synthesis and structure-activity relationship of a series of substituted piperidinyl glycine 2-cyano-4,5-methano pyrroline DPP-IV inhibitors are described. Improvement of the inhibitory activity and chemical stability of this series of compounds was respectively achieved by the introduction of bulky groups at the 4-position and 1-position of the piperidinyl glycine, leading to a series of potent and stable DPP-IV inhibitors.
        
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Zhao G, Kwon C, Wang A, Robertson JG, Marcinkeviciene J, Parker RA, Kirby MS, Hamann LG (2013) Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors Bioorganic & Medicinal Chemistry Lett23: 1622-5
Zhao G, Kwon C, Wang A, Robertson JG, Marcinkeviciene J, Parker RA, Kirby MS, Hamann LG (2013) Bioorganic & Medicinal Chemistry Lett23: 1622-5