📜3-苯基丙基硫代异氰酸酯,L-半胱氨酸盐酸盐无水物置于sodium Hydroxide体系中,用 乙醇,水 用作溶剂,化学反应 48.0H,以95%的收率获得s-[n-(3-苯丙基)氨基硫羰基]-L-半胱氨酸
参考文献:Phenylalkyl Isothiocyanate-Cysteine Conjugates As Glutathione S-Transferase Stimulating Agents
标题:Phenylalkyl Isothiocyanate-Cysteine Conjugates As Glutathione S-Transferase Stimulating Agents
摘要:To Develop Analogues Of Phenylalkyl Isothiocyanate With Less Toxicity And Better Biological Activity,Two Water-Soluble Phenylalkyl Isothiocyanate-Cysteine Conjugates,S-[n-Benzyl(Thiocarbamoyl)]-L-Cysteine (1) And S-[n-(3-Phenylpropyl)Thiocarbamoyl)]-L-Cysteine (2),Were Synthesized. The Induction Of Increased Activity Of The Detoxifying Enzyme Glutathione S-Transferase By The Conjugates And Their Parent Compounds Was Determined And Compared In Several Tissues Of A/j Mice. The Biological Evaluation Revealed That The Conjugates As Gst Enzyme Inducers Appeared To Be Less Toxic And Even More Potent Than The Parent Compounds In The Mouse Bladder. Compounds 1 Was Much More Active Than 2 In All The Tissues Examined,While Their Parent Compounds Showed An Inverse Order Of Activity. Thus,An Increase In The Alkyl Chain Length Of The Parent Isothiocyanates Or A Decrease In The Alkyl Length Of The Conjugates Could Result In Higher Enzyme-Inducing Activity M The Same Compound Series. Since A Number Of Nitrosamines Have Been Identified As Prime Bladder Carcinogens And Phenylalkyl Isothiocyanates Have Been Reported To Inhibit A Wide Range Of Carcinogenic Nitrosamines,The Corresponding Conjugates May Serve As Prodrugs To Protect Against Nitrosamine-Induced Urinary Bladder Carcinogenesis Once They Are Delivered To The Target Organ.
Doi:10.1021/jm00079A025