CAS: 180001-34-7; N-(3-(Aminomethyl)Benzyl)Acetimidamide

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CAS号108467-99-8 N-[3-(氨基甲基)苄基]氨...

📜N-[3-(氨基甲基)苄基]氨基甲酸叔丁酯置于盐酸体系中,用 1,4-二氧六环,乙醇 用作溶剂,化学反应 6.0H,反应生成N-[3-(氨甲基)苄基]乙脒
参考文献:Mechanism Of Inactivation Of Inducible Nitric Oxide Synthase By Amidines. Irreversible Enzyme Inactivation Without Inactivator Modification
标题:Mechanism Of Inactivation Of Inducible Nitric Oxide Synthase By Amidines. Irreversible Enzyme Inactivation Without Inactivator Modification
摘要:Nitric Oxide Synthases (Nos) Are Hemoproteins That Catalyze The Reaction Of L-Arginine To L-Citrulline And Nitric Oxide. N-(3-(Aminomethyl)Benzyl)Acetamidine (1400W) Was Reported To Be A Slow,Tight-Binding,And Highly Selective Inhibitor Of Inos In Vitro And In Vivo. Previous Mechanistic Studies Reported That 1400W Was Recovered Quantitatively After Inos Fully Lost Its Activity And Modification To Inos Was Not Detected. Here,It Is Shown That 1400W Is A Time-,Concentration-,And Nadph-Dependent Irreversible Inactivator Of Inos. HPLC-Electrospray Mass Spectrometric Analysis Of The Incubation Mixture Of Inos With 1400W Shows Both Loss Of Heme Cofactor And Formation Of Bilivedin,As Was Previously Observed For Inos Inactivation By Another Amidine-Containing Compound,N-5(1-Iminoethyl)-L-Ornithine (L-Nio). The Amount Of Biliverdin Produced Corresponds To The Amount Of Heme Lost By 1400W Inactivation Of Inos. A Convenient Ms/ms-HPLC Methodology Was Developed To Identify The Trace Amount Of Biliverdin Produced By Inactivation Of Inos With Either 1400W Or L-Nio To Be Biliverdin \xalpha Out Of The Four Possible Regioisomers. Two Mechanisms Were Previously Proposed For Inos Inactivation By L-Nio: (1) Uncoupling Of The Heme Peroxide Intermediate,Leading To Destruction Of The Heme To Biliverdin; (2) Abstraction Of A Hydrogen Atom From The Amidine Methyl Group Followed By Attachment To The Heme Cofactor,Which Causes The Enzyme To Catalyze The Heme Oxygenase Reaction. The Second Mechanistic Proposal Was Ruled Out By Inactivation Of Inos With D(3)-1400W,Which Produced No D(2)-1400W. Detection Of Carbon Monoxide As One Of The Heme-Degradation Products Further Excludes The Covalent Heme Adduct Mechanism. On The Basis Of These Results,A Third Mechanism Is Proposed In Which The Amidine Inactivators Of Inos Bind As Does Substrate L-Arginine,But Because Of The Amidine Methyl Group,The Heme Peroxy Intermediate Cannot Be Protonated,Thereby Preventing Its Conversion To The Heme Oxo Intermediate. This Leads To A Change In The Enzyme Mechanism To One That Resembles That Of Heme Oxygenase,An Enzyme Known To Convert Heme To Biliverdin \xalpha.. This Appears To Be The First Example Of A Compound That Causes Irreversible Inactivation Of An Enzyme Without Itself Becoming Modified In Any Way.
Doi:10.1021/ja0445645

专利信息

专利号:US-2009325858-A1
优先权日:2003-03-21
标 题:Reduction of Zinc-Induced Neurotoxic Injury By Blockade of Nitric Oxide Synthesis
发明人：FREDERICKSON CHRISTOPHER J
权利人:ANDRO DIAGNOSTICS INC
摘要:The present invention provides methods of inhibiting release of zinc from neurons and of preventing zinc-mediated brain injury. Also provided are methods of improving cerebral blood flow while preventing zinc-mediated brain injury. Inhibitors of or activators of nitric oxide synthases modulate nitric oxide synthesis to reduce nitric oxide-induced release of neurotoxic amounts of zinc, thereby reducing zinc-mediated neuronal injury after brain trauma.

专利号:US-12294050-B2
优先权日:2014-12-02
标 题 :Lithium ion conducting sulfide glass fabrication
发明人：VISCO STEVEN J; PETROV ALEXEI; LOGINOVA VALENTINA; NIMON VITALIY; NIMON YEVGENIY S; KATZ BRUCE D
权利人:POLYPLUS BATTERY CO INC
摘要:Preparation of anhydrous lithium sulfide (Li2S) purified suitably for applications in advanced batteries, and, in particular, for synthesis of solid electrolytes based on Li2S, including sulfide solid electrolytes of the type that may be described as crystalline (e.g., polycrystalline), amorphous (e.g., glass) and combinations thereof, such as sulfide glass-ceramic solid electrolyte materials.

专利号:US-2010278751-A1
优先权日:2009-04-30
标题 :Radiolabeled 2-amino-4-alkyl-6-(haloalkyl)pyridine compounds and their use in diagnostic imaging
发明人：MACH ROBERT H; ZHOU DONG; WELCH MICHAEL
权利人:UNIV WASHINGTON
摘要:Radiolabeled 2-amino-4-alkyl-6-(haloalkyl)pyridine compounds are disclosed. In some aspects, the compounds bind to inducible nitric oxide synthase (iNOS) with high specificity. In some configurations, a compound comprising a radioisotope can be used for diagnostic imaging of iNOS distribution in a mammalian subject such as a human, using a scanning method such as positron emission tomography (PET scanning). Methods of synthesis of the compounds are also disclosed.

专利号:US-2005032691-A1
优先权日:2000-02-08
标 题 :Methods for treating glaucoma
发明人：WAX MARTIN B; TEZEL GULGUN
摘要:This invention provides a method for treating a subject with glaucoma comprising the steps of administrating a compound or composition which antagonize, inhibits, inactivates, reduce, suppresses, antagonizes, and/or limits the release, synthesis, or production from cells of TNF-α thereby treating the subject with glaucoma.

专利号:US-2004235751-A1
优先权日:2003-03-21
标题 :Reduction of zinc-induced neurotoxic injury by blockade of nitric oxide synthesis

专利号:WO-2024010355-A1
优先权日:2022-07-07
标 题:Anti-aging composition containing extract from gosori wine lees
发明人：WOO JI EUN; SHIN SEOUNG WOO; CHO EUN AE; JUNG EUN SUN; CHO SHIN HWAN; KIM MYEONG OK; PARK DEOK HOON
权利人:BIOSPECTRUM INC; SKINCURE INC
摘要:The present invention relates to an anti-aging composition containing an extract from Gosori wine lees. The extract from the Gosori wine lees can be advantageously used as a cosmetic material as it not only has the effects of inhibiting cellular aging caused by oxidative stress, promoting collagen synthesis, suppressing elastase activity, inhibiting inflammatory substance secretion, stimulating sebum production, and providing skin whitening simultaneously, thus allowing for effective prevention and alleviation of skin aging, but also is free from skin irritation and exhibits excellent safety for the human body.