CAS: 19227-14-6; 4-Bromo-N-Hydroxybenzimidamide

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📜4-溴苯腈置于吡啶,盐酸羟胺体系中,用 乙醇 用作溶剂,化学反应生成(E)-4-溴-N'-羟基苄脒
参考文献:哌啶-螺恶二唑衍生物作为α7烟碱样受体拮抗剂的设计,合成和生物学活性.
标题:哌啶-螺恶二唑衍生物作为α7烟碱样受体拮抗剂的设计,合成和生物学活性.
摘要:α 已经提出在神经和免疫系统中表达的7种烟碱乙酰胆碱受体(nachrs)在炎症控制中起重要作用.然而,由于缺乏的拮抗剂工具特异性抑制α 7个的nachr阻碍通道作为治疗靶的验证.要发现的选择性α 7拮抗剂,我们开始了基于药效的虚拟筛选和鉴定的哌啶衍生物spirooxadiazole T761-0184充当α 7拮抗剂.随后在非洲爪蟾卵母细胞中合成了一系列新型哌啶-螺二恶唑衍生物,并使用两电极电压钳(tevc)分析对其进行了评估.两个系列的铅化合物均受抑制α7的ic 50值为3.3μm至13.7μm.化合物b10表现出α 7选择性超过其它α 4 β 2和α 3 β 4的nachr亚型.的结构-活性关系的分析(sar)提供了一种用于选择性的进一步发展了有价值的见解α 7的nachr拮抗剂.
Doi:10.1016/j.Ejmech.2020.112774

专利信息

专利号:US-7071338-B2
优先权日:2002-11-27
标 题 :Process for the synthesis of bis-aryl diamidoxime compounds
发明人：BOYKIN DAVID W; ANBAZHAGAN MARIAPPAN; TIDWELL RICHARD R
权利人:UNIV GEORGIA STATE RES FOUND
摘要:Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.

专利号:WO-2023141114-A2
优先权日:2022-01-18
标 题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives

专利号:US-2004127721-A1
优先权日:2002-11-27
标 题 :Process for the synthesis of bis-aryl diamidoxime compounds