CAS: 16120-92-6; (S)-2-Amino-4-(Methylthio)Butanamide Hydrochloride

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4510-08-1 52811-68-4 197893-07-5

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CAS号6810-12-4 L-甲硫氨酸盐酸盐 溶液 | CAS号34805-23-7 N-tert-butoxyca... | CAS号2488-15-5 B°C-L-蛋氨酸

Boc-L-蛋氨酸置于盐酸,Ammonium Hydroxide体系中,用 溶剂黄146 用作溶剂,化学反应 1.0H,反应生成L-蛋氨酰胺
参考文献:Synthesis And Biological Evaluation Of Dehydrophenylalanine Containing Substance P Fragments
标题:Synthesis And Biological Evaluation Of Dehydrophenylalanine Containing Substance P Fragments
摘要:合成了与物质p的c端片段(6-11)和(4-11)相对应的肽段,这些片段包含一个假定的β-转角,采用溶液相的方法.合成了物质p的类似物,其中第8位的苯丙氨酸残基被脱氢苯丙氨酸(δphe)替代,第9位的甘氨酸残基被丙氨酸,缬氨酸,肌氨酸(n-me-gly)和α-氨基异丁酸替代.在两个类似物[8-δphe,9-Sar]-sp (4-11) (5)和[5,8-δphe,9-Aib]-sp (4-11) (7)中,第5位的谷氨酰胺残基也被δphe替代.这些类似物在豚鼠回肠制备中(体外)评估了其引起平滑肌收缩的能力,并在以氨基甲酸酯麻醉的雌性大鼠中评估了其降血压活性.在六肽系列中,[8-δphe]-sp (6-11) (1)和[8-δphe,9-Sar]-sp (6-11) (4)在两项实验中均显示出显著的活性.八肽[5,8-δphe,9-Sar]-sp (4-11) (5)在第5和第8位具有δphe残基并在第9位含有肌氨酸,发现其在体外和体内系统中是最有效的类似物.
Doi:10.1246/bcsj.65.3412

专利信息

专利号:CH-422814-A
优先权日:1961-06-08
标 题 :Process for the synthesis of alpha-amino acid amide halohydrates

专利号:US-5663149-A
优先权日:1994-12-13
标 题:Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
发明人：PETTIT GEORGE R; SRIRANGAM JAYARAM K; KANTOCI DARKO
权利人:UNIV ARIZONA
摘要:The synthesis and elucidation of nineteen heterocyclic or halophenyl amideerivatives of dolastatin 10 are disclosed. These compounds and the methods of producing those compounds offer demonstrated significant in vitro activity against several human cancer cell lines. These compounds and the methods of producing those compounds offer a commercially viable alternative to natural and synthetic dolastatin 10.