title: [Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors].
abstract: To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.
authors.affiliation: Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China.
authors.forename: Bei
authors.initials: B
authors.lastname: Han
authors.forename: Yi
authors.initials: Y
authors.lastname: Huan
authors.forename: Zi-Yun
authors.initials: ZY
authors.lastname: Lin
authors.forename: Peng
authors.initials: P
authors.lastname: Li
authors.forename: Zhu-Fang
authors.initials: ZF
authors.lastname: Shen
authors.forename: Da-Li
authors.initials: DL
authors.lastname: Yin
authors.forename: Hai-Hong
authors.initials: HH
authors.lastname: Huang
mesh_terms: D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D010879:Piperazines; C018556:glycine amide; C014886:1-ethyl-2,3-dioxopiperazine; D018819:Dipeptidyl Peptidase 4; D005998:Glycine