CAS: 160729-91-9; (2S)-1-[(2S,4R)-4-Benzyl-2-Hydroxy-5-[[(1S,2R)-2-Hydroxy-2,3-Dihydro-1H-Inden-1-Yl]Amino]-5-Oxopentyl]-N-Tert-Butyl-4-(Furo[2,3-B]Pyridin-5-Ylmethyl)Piperazine-2-Carboxamide

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[14C]-N-Dealkyl Indinavir 5-(chloromethyl)furo[2,3-b]pyridine

📜[1(1S,2R),5(S)]-2,3,5-三脱氧-N-(2,3-二氢-2-羟基-1H-茚-1-基)-5-[2-[(叔丁基氨基)甲酰]-1-哌嗪基]-2-(苯基甲基)-D-赤式-戊酰胺,5-(Chloromethyl)Furo[2,3-B]Pyridine置于三乙胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 48.0H,以84%的收率获得人参皂苷ck
参考文献:Identification Of Mk-944A: A Second Clinical Candidate From The Hydroxylaminepentanamide Isostere Series Of Hiv Protease Inhibitors
标题:Identification Of Mk-944A: A Second Clinical Candidate From The Hydroxylaminepentanamide Isostere Series Of Hiv Protease Inhibitors
摘要:Recent Results From Human Clinical Trials Have Established The Critical Role Of Hiv Protease Inhibitors In The Treatment Of Acquired Immune-Deficiency Syndrome (Aids). However,The Emergence Of Viral Resistance,Demanding Treatment Protocols,And Adverse Side Effects Have Exposed The Urgent Need For A Second Generation Of Hiv Protease Inhibitors. The Continued Exploration Of Our Hydroxylaminepentanamide (Hapa) Transition-State Isostere Series Of Hiv Protease Inhibitors,Which Initially Resulted In The Identification Of Crixivan (Indinavir Sulfate,Mk-639,L-735,524),Has Now Yielded Mk-944A (L-756,423). This Compound Is Potent,Is Selective,And Competitively Inhibits Hiv-1 Pr With A Ki Value Of 0.049 Nm. It Stops The Spread Of The Hiviiib-Infected Mt4 Lymphoid Cells At 25.0-50.0 Nm,Even In The Presence Of Alpha(1) Acid Glycoprotein,Human Serum Albumin,Normal Human Serum,Or Fetal Bovine Serum. Mk-944A Has A Longer Half-Life In Several Animal Models (Rats,Dogs,And Monkeys) Than Indinavir Sulfate And Is Currently In Advanced Human Clinical Trials.
Doi:10.1021/jm9903848