CAS: 57184-23-3; 1-(Cyclohexylmethyl)Piperazine

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27561-62-2 412293-90-4 90754-63-5

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CAS号1206676-28-9 4-Cyclohexylmet... | CAS号2550-36-9 溴甲基环己烷 | CAS号2043-61-0 环己烷甲醛 | CAS号7755-92-2 N-甲酰基哌嗪

T-Butyl 4-(Cyclohexylmethyl)Piperazine-1-Carboxylate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,反应生成 1-环己甲基哌嗪
参考文献:发现新型芹菜素-哌嗪杂合体作为有效的选择性聚(adp-核糖)聚合酶-1(parp-1)抑制剂用于治疗癌症
标题:发现新型芹菜素-哌嗪杂合体作为有效的选择性聚(adp-核糖)聚合酶-1(parp-1)抑制剂用于治疗癌症
摘要:聚(adp-核糖)聚合酶-1 (Parp-1) 是发现化学增敏剂和抗癌药物的潜在靶标.据报道,Amentoflavone (Amf) 是一种选择性 Parp-1 抑制剂.在这里,Amf的结构修饰和修剪分别产生了一系列amf衍生物 (9A-h) 和芹菜素-哌嗪/哌啶杂化物 (14A-p,15A-p,17A-h和19A-f).在这些化合物中,15L表现出有效的parp-1抑制作用(ic 50 = 14.7 Nm),并且对parp-1的选择性高于对parp-2的选择性(61.2倍).分子动力学模拟和细胞热位移测定表明15L直接与parp-1结构结合.在体外和体内研究中,15L对 A549 细胞显示出有效的化疗增敏作用,并通过 Parp-1 抑制对 Sk-Ov-3 细胞具有选择性细胞毒作用. 15L.2Hcl还表现出非常好的 Adme 特性,药代动力学参数和理想的安全裕度.
DOI:10.1021/acs.Jmedchem.1C00735

专利信息

专利号:US-4301129-A
优先权日:1978-09-18
标题 :Synthesis of NaBH3 CN and related compounds
发明人：WADE ROBERT C; HUI BENJAMIN C
权利人:THIOKOL CORP
摘要:A process for the preparation of compounds of the formula RBH 3 CN wherein R is an alkali metal, a quaternary ammonium radical or a phosphonium radical wherein a compound of the formula RCN is treated with a stoichiometric amount or slightly less than a stoichiometric amount of a BH 3 donor is described. The final products are useful as hydrolysis stable reductants and as synthetic intermediates.

专利号:RU-2041210-C1
优先权日:1989-11-01
标题:Method of synthesis of imidazo-(4,5-b)-quinolinylhydroxyalkanoic acid amides or their pharmaceutically used salts

专利号:RU-2129554-C1
优先权日:1993-06-21
标题:Derivatives of pyrrolequinolinone, method of their synthesis, intermediate compounds for their synthesis, pharmaceutical composition and method of its preparing

专利号:US-11731947-B2
优先权日:2019-04-10
标题:Deuterated antimicrobial compounds
发明人：MILLER MARVIN J; KRCHNAK VIKTOR; LIU RUI
权利人:UNIV NOTRE DAME DU LAC
摘要:Substituted nitrobenzothiazinones (BTZs) are potent antituberculosis prodrugs that are reductively activated to produce nitroso moieties that form covalent adducts with a cysteine residue of decaprenylphosphoryl-β-D-ribose-2′-oxi-dase (DprE1) of Mycobacterium tuberculosis (Mtb). The resulting cell wall synthesis inhibition is lethal to Mtb, leading to consideration of development of BTZs for clinical use. The hydride-induced reduction of the nitroaromatic proceeds by reversible formation of the corresponding Meisenheimer complex. Herein we demonstrate that chemical reduction of BTZ043 with NaBD4 followed by reoxidation incorporates deuterium into the core nitro aromatic warhead. Subsequent reduction of the deuterated species is not affected, but, as expected, reoxidation is slowed by the deuterium isotope effect, thus prolonging the lifetime of the active nitroso oxidation state.