title: Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors.
abstract: 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.
authors: Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA. guohua.zhao@bms.com
authors: Guohua
authors: G
authors: Zhao
authors: Chet
authors: C
authors: Kwon
authors: Aiying
authors: A
authors: Wang
authors: James G
authors: JG
authors: Robertson
authors: Jovita
authors: J
authors: Marcinkeviciene
authors: Rex A
authors: RA
authors: Parker
authors: Mark S
authors: MS
authors: Kirby
authors: Lawrence G
authors: LG
authors: Hamann
mesh_terms: D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry* / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D010880:Piperidines / Q000737:chemistry*; D011485:Protein Binding; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013696:Temperature
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D010880:Piperidines; D011759:Pyrrolidines; C032727:piperidine; D018819:Dipeptidyl Peptidase 4