CAS: 53348-92-8; 4-Amino-2H-Chromen-2-One

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CAS号1076-38-6 4-羟基香豆素; 4-羟基-1... | CAS号118-93-4 邻羟基苯乙酮 | CAS号138313-74-3 5H-[1]Benzopyra... | CAS号138313-73-2 5H-[1]Benzopyra... | CAS号138313-75-4 5H-[1]Benzopyra... | CAS号138313-72-1 5H-[1]Benzopyra... | CAS号138313-71-0 5H-[1]Benzopyra... | CAS号138313-68-5 2H-[1]Benzopyra... | CAS号4812-86-6 1-(4-amino-3,5-...

📜4-羟基香豆素置于ammonium Acetate体系中,化学反应 5.0H,以77%的收率获得产物4-氨基-苯并吡喃-2-酮
参考文献:基于4-氨基香豆素的芳香硫脲作为潜在的杰克豆脲酶抑制剂;合成,酶抑制动力学和对接研究
标题:基于4-氨基香豆素的芳香硫脲作为潜在的杰克豆脲酶抑制剂;合成,酶抑制动力学和对接研究
摘要:背景:脲酶会催化尿素水解成氨和二氧化碳,过量的氨会导致全球变暖和农作物减产.尿素还引起某些人类疾病,例如胃癌,消化性溃疡,肾盂肾炎和肾结石.开发了新的脲酶抑制剂以消除此类问题. 目的:本文描述了一系列作为杰克豆脲酶抑制剂的新型1-芳基-3-(2-Oxo-2H-Chromen-4-基)硫脲衍生物(5A-J)的合成. 方法:将新鲜制备的异硫氰酸芳基酯与4-氨基香豆素在同一罐中于无水丙酮介质中反应.标题硫脲(5A-J)的结构通过其光谱数据确定.确定了对杰克豆脲酶的抑制作用. 结果:发现化合物5I和5J表现出优异的活性,Ic50分别为0.0065和0.0293,µm.带有4-甲基取代的苯环的化合物5I在酶抑制活性中起着至关重要的作用.通过lineweavere-Burk图分析的动力学机理表明,化合物5I非竞争性抑制酶.根据lineweavere-Burk图计算的化合物5I的michaelis-Menten常数km和抑制常数ki分别为4
DOI:10.2174/1573406415666190715164834

专利信息

专利号:US-9802890-B2
优先权日:2006-02-21
标 题 :Processes for the convergent synthesis of calicheamicin derivatives
发明人：MORAN JUSTIN KEITH; GU JIANXIN
权利人:WYETH LLC
摘要:This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.

专利号:US-5877296-A
优先权日:1994-06-03
标题:Process for preparing conjugates of methyltrithio antitumor agents
发明人：HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN
权利人:AMERICAN CYANAMID CO
摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

专利号:US-5739116-A
优先权日:1994-06-03
标题:Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents

专利号:US-2007197455-A1
优先权日:2006-02-21
标 题:Processes for the convergent synthesis of calicheamicin derivatives

专利号:US-2009312530-A1
优先权日:2006-02-21
标题:Processes for the convergent synthesis of calicheamicin derivatives

专利号:US-8273862-B2
优先权日:2006-02-21
标题:Processes for the convergent synthesis of calicheamicin derivatives