CAS: 913980-23-1; (S)-1-(2-Aminoacetyl)Pyrrolidine-2-Carbonitrile Hydrochloride

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704-15-4 207557-35-5 914070-99-8

📜L-脯氨酰胺置于吡啶,N,N-二异丙基乙胺,三氟乙酸酐,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺,乙腈 作为反应溶剂,化学反应 28.5H,反应生成 维格列汀杂质57
参考文献:Selective Inhibitors Of Fibroblast Activation Protein (Fap) With A (4-Quinolinoyl)-Glycyl-2-Cyanopyrrolidine Scaffold
标题:Selective Inhibitors Of Fibroblast Activation Protein (Fap) With A (4-Quinolinoyl)-Glycyl-2-Cyanopyrrolidine Scaffold
摘要:Fibroblast Activation Protein (Fap) Is A Serine Protease That Is Generally Accepted To Play An Important Role In Tumor Growth And Other Diseases Involving Tissue Remodeling. Currently There Are No Fap Inhibitors With Reported Selectivity Toward Both The Closely Related Dipeptidyl Peptidases (Dpps) And Prolyl Oligopeptidase (Prep). We Present The Discovery Of A New Class Of Fap Inhibitors With A N-(4-Quinolinoyl)-Gly-(2-Cyanopyrrolidine) Scaffold. We Have Explored The Effects Of Substituting The Quinoline Ring And Varying The Position Of Its Sp(2) Hybridized Nitrogen Atom. The Most Promising Inhibitors Combined Low Nanomolar Fap Inhibition And High Selectivity Indices (>10(3)) With Respect To Both The Dpps And Prep. Preliminary Experiments On A Representative Inhibitor Demonstrate That Plasma Stability,Kinetic Solubility,And Log D Of This Class Of Compounds Can Be Expected To Be Satisfactory.
DOI:10.1021/ml300410D