CAS: 18465-28-6; 3-Methyl-Benzamidine

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3-Methylbenzonitrile 4-Benzylidene-2-m-tolyl-2-imidazolin-5-one N-[imino(3-methylphenyl)methyl]-2-nitrobenzamide N-[imino(3-methylphenyl)methyl]-5-methyl-2-nitrobenzamide

📜间甲基苯腈置于乙醇,乙酰氯,Sodium,氯化铵体系中,用 乙酸乙酯,甲醇 用作溶剂,化学反应 24.0H,反应生成3-甲基苯甲酰胺
参考文献:抗恶性黑色素瘤的新型脱氧马尿苷合酶变构抑制剂:设计,合成和生物学评价
标题:抗恶性黑色素瘤的新型脱氧马尿苷合酶变构抑制剂:设计,合成和生物学评价
摘要:基于脱氧马尿苷合酶(Dhps)的新型变构位点,设计并合成了两个系列的30种新型5-(2-甲氧基苯氧基)-2-苯基嘧啶-4-胺衍生物作为dhps抑制剂.其中,化合物8M的dhps抑制效力最好(ic 50 = 0.014 μm),对黑色素瘤细胞表现出优异的抑制作用,优于gc7.此外,分子对接和分子动力学(md)模拟进一步证明化合物8M与dhps的变构位点紧密结合.流式细胞术分析和酶联免疫吸附测定(elisa)表明化合物8M可以抑制细胞内活性氧(ros)水平.此外,通过蛋白质印迹分析,化合物8M有效激活caspase 3并降低gp-100,酪氨酸酶,Eif5A2,Mmp2和mmp9的表达.此外,Transwell分析和伤口愈合分析均表明化合物8M可以抑制黑色素瘤细胞的侵袭和迁移.在体内研究中,肿瘤异种移植模型表明,化合物8M能有效抑制黑色素瘤的发展,且毒性低.
Doi:10.1021/acs.Jmedchem.1C00582

专利信息

专利号:US-9126942-B2
优先权日:2008-03-08
标题 :Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists
发明人：VAN LOEVEZIJN ARNOLD; IWEMA BAKKER WOUTER I; STOIT ALEX; RENSINK AGATHA M; VENHORST JENNIFER; VAN DER NEUT MARTINA A W; DE HAAN MARTIN; KRUSE CORNELIS G
权利人:ABBVIE BAHAMAS LTD
摘要:This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

专利号:CN-107311994-A
优先权日:2017-08-14
标题 :A novel synthesis method of S1P‑1 receptor agonist drug molecule