CAS: 40615-04-1; 3-(Aminomethyl)Benzo[b]Thiophene

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benzo[b]thiophene-3-carbaldehyde oxime benzo[b]thiophene-3-carboxylic acid benzothiophene-3-carbonyl chloride 3-benzothiophenecarboxamide Benzo[b]thiophen-3-ylmethyl-((E)-3-phenyl-allyl)-amine thiophenemethanamine(E)-N-methyl-N-(3-phenyl-2-propenyl)-3-benzothiophenemethanamine 2-bromo-5-fluoropyridine 2-ethynyl-5-fluoropyridine

📜1-苯并噻吩-3-羧酸置于ammonium Hydroxide,Lithium Aluminium Tetrahydride,氯化亚砜体系中,用 四氢呋喃,二氯甲烷,水,甲苯 作为反应溶剂,化学反应 7.0H,反应生成 3-氨甲基苯并噻吩
参考文献:设计和合成基于杂芳基的苯磺酰胺衍生物作为h5N1甲型流感病毒的有效抑制剂†
标题:设计和合成基于杂芳基的苯磺酰胺衍生物作为h5N1甲型流感病毒的有效抑制剂†
摘要:甲型流感病毒是一种包膜的负性单链rna病毒,可引起发热的呼吸道感染,对人类健康乃至全世界的生命都构成了具有临床挑战性的威胁.更令人震惊的是高致病性禽流感(hpai)菌株(如h5N1)的出现,其在人类感染中的死亡率(60%)比季节性流感菌株高得多.在这项研究中,新的杂芳基苯磺酰胺衍生物系列被确定为m2质子通道抑制剂.对结构-活性关系的系统研究和分子对接研究表明,磺酰胺部分和2,5-二甲基取代的噻吩作为核心结构在抗流感活性中起着重要作用.在衍生物中,化合物11K具有对h5N1病毒的优异抗病毒活性,Ec 50值为0.47μm,选择性指数为119.9,与参考药物金刚烷胺相当.
DOI:10.1039/c8Md00474A

专利信息

专利号:US-7179918-B2
优先权日:2001-06-11
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.