CAS: 13182-89-3; 2-(2-Methyl-5-Nitro-1H-Imidazol-1-yl)Ethyl Benzoate

上下游产品

metronidazole benzoic acid benzoyl chloride toluene-4-sulfonic acid 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl estermetronidazole benzoic acid 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 2-chloro-4,5-difluorobenzoate 16H19N3O4C16H19N3O4

甲硝唑置于吡啶,Potassium Carbonate体系中,用 氯仿,N,N-二甲基甲酰胺 用作溶剂,化学反应 96.0H,反应生成苯酰甲硝唑
参考文献:甲硝唑芳氧基,羧基和吡咯衍生物:合成,抗肿瘤活性,Qsar,分子对接和动力学研究
标题:甲硝唑芳氧基,羧基和吡咯衍生物:合成,抗肿瘤活性,Qsar,分子对接和动力学研究
摘要:已经合成了一系列新颖的甲硝唑芳氧基,羧基和唑衍生物,并通过mtt分析评估了它们对三种癌细胞系的细胞毒活性.化合物4M,4L和4D表现出最强的细胞毒活性(ic 50小于100 µg / Ml).还通过流式细胞术检测了这些化合物的凋亡.进行了对接研究以提出可能的靶蛋白.下一步,对与化合物4M结合的拟议目标蛋白粘着斑激酶(fak,Pdb代码:2Etm)进行了分子动力学模拟.As,4M 提示其具有强力的细胞毒活性和可接受的凋亡作用,它可能是潜在的抗癌候选药物,可以通过抑制fak发挥作用.
Doi:10.1016/j.Bmc.2018.12.003

专利信息

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:CN-102382061-A
优先权日:2011-11-07
标 题:Synthesis of Benzoyl Ornidazole