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4-[5-(乙酰氨基甲基)呋喃-2-基]-2-氨基噻唑 | 150208-26-7

中文名称
4-[5-(乙酰氨基甲基)呋喃-2-基]-2-氨基噻唑
中文别名
N-{[5-(2-氨基-1,3-噻唑-4-基)-2-呋喃基]甲基}乙酰胺
英文名称
N-[[5-(2-aminothiazol-4-yl)-2-furyl]methyl]acetamide
英文别名
4-[5-(acetamidomethyl)furan-2-yl]-2-aminothiazole;N-{[5-(2-amino-1,3-thiazol-4-yl)furan-2-yl]methyl}acetamide;N-[[5-(2-amino-1,3-thiazol-4-yl)furan-2-yl]methyl]acetamide
4-[5-(乙酰氨基甲基)呋喃-2-基]-2-氨基噻唑化学式
CAS
150208-26-7
化学式
C10H11N3O2S
mdl
MFCD07838302
分子量
237.282
InChiKey
HMOORGLQDZENJJ-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    0.5
  • 重原子数:
    16
  • 可旋转键数:
    3
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    0.2
  • 拓扑面积:
    109
  • 氢给体数:
    2
  • 氢受体数:
    5

上下游信息

  • 下游产品
    中文名称 英文名称 CAS号 化学式 分子量

反应信息

  • 作为反应物:
    参考文献:
    名称:
    Anti- Helicobacter pylori agents. 2. Structure activity relationships in a new series of 2-alkylguanidino-4-furylthiazoles
    摘要:
    SAR for antimicrobial activity against H. pylori was investigated in a new series of 2-alkylguanidino-4-furylthiazoles. Of the compounds obtained, cyclohexylmethyl and ethoxyethyl derivatives were identified as a novel class of anti-H. pylori agents which possessed potent and selective antimicrobial activity against H. pylori. These compounds also showed gastric antisecretory activity. (C) 1998 Elsevier Science Ltd. All rights reserved.
    DOI:
    10.1016/s0960-894x(98)00206-6
  • 作为产物:
    参考文献:
    名称:
    Anti- Helicobacter pylori agents. 2. Structure activity relationships in a new series of 2-alkylguanidino-4-furylthiazoles
    摘要:
    SAR for antimicrobial activity against H. pylori was investigated in a new series of 2-alkylguanidino-4-furylthiazoles. Of the compounds obtained, cyclohexylmethyl and ethoxyethyl derivatives were identified as a novel class of anti-H. pylori agents which possessed potent and selective antimicrobial activity against H. pylori. These compounds also showed gastric antisecretory activity. (C) 1998 Elsevier Science Ltd. All rights reserved.
    DOI:
    10.1016/s0960-894x(98)00206-6
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文献信息

  • [EN] BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY<br/>[FR] AMIDES DE BENZOFURANE ET LEURS ANALOGUES HÉTÉROAROMATIQUES DESTINÉS À ÊTRE UTILISÉS EN THÉRAPIE
    申请人:EUROPEAN MOLECULAR BIOLOGY LABORATORY
    公开号:WO2018229193A1
    公开(公告)日:2018-12-20
    The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- maceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, and to certain novel compoundsof the formula Ias described below or a tautomer or a pharmaceuti- cally acceptable salt thereof. Formula (I) wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; with the proviso that at most two of X1, X2, X3 and X4 are N; L1, L2 are a bond or a bivalent radical such as C1-C6-alkylene or C3-C8-cycloalkylene; A is 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated carbocyclic ring which may carry one or more substituents R9; or L2-A forms a group C1-C6-alkylene-OR13, C1-C6-alkylene-SR14 or C1-C6-alkylene-NR15R16; and R1, R2, R3, R4, R5, R6, R9, R13, R14, R15 and R16 are as defined in the claims and the description.
    本发明涉及一种药物组合物,包括下述的化合物I的构造或其互变异构体或药用盐;以及用作药物的下述的化合物I的构造或其互变异构体或药用盐,特别用于治疗或预防从炎症性疾病、过度增殖性疾病或紊乱、缺氧相关病理和以过度血管生成为特征的疾病中选择的疾病或紊乱;以及下述的某些新型化合物I的构造或其互变异构体或药用盐。其中,化合物(I)中X1为CR1或N;X2为CR2或N;X3为CR3或N;X4为CR4或N;但X1、X2、X3和X4中最多有两个为N;L1、L2为键或类似C1-C6-烷基或C3-C8-环烷基的二价基团;A为3-、4-、5-、6-、7-或8-成员饱和、部分不饱和或最大不饱和的碳环,可能携带一个或多个取代基R9;或L2-A形成一个基团C1-C6-烷基-OR13、C1-C6-烷基-SR14或C1-C6-烷基-NR15R16;而R1、R2、R3、R4、R5、R6、R9、R13、R14、R15和R16如权利要求和说明中所定义。
  • Anti-<i>Helicobacter pylori</i> Agents. 1. 2-(Alkylguanidino)-4-furylthiazoles and Related Compounds
    作者:Yousuke Katsura、Tetsuo Tomishi、Yoshikazu Inoue、Kazuo Sakane、Yoshimi Matsumoto、Hirohumi Ishikawa、Hisashi Takasugi
    DOI:10.1021/jm970407n
    日期:1997.8.1
    les and related compounds were synthesized and evaluated for antimicrobial activity against Helicobacter pylori, inhibitory effect on gastric acid secretion, and histamine H2-receptor antagonist activity. Introduction of alkyl substituents on the guanidino moiety resulted in a significant increase in antimicrobial activity, which was associated with the alkyl chain length. Of the compounds obtained
    合成了一系列2-(烷基胍基)-4- [5-(乙酰氨基甲基)呋喃-2-基]噻唑及其相关化合物,并评估了其对幽门螺杆菌的抗菌活性,对胃酸分泌的抑制作用以及组胺H2-受体的抑制作用。拮抗剂活性。在胍基部分上引入烷基取代基导致抗菌活性显着增加,这与烷基链长有关。在获得的化合物中,正己基胍基衍生物13的活性(MIC = 0.11微克/ mL)比未取代的胍基衍生物7提高了250倍。烷基取代的胍基衍生物还显示出胃的抗分泌和H2拮抗剂活性。然而,在这些测定中未发现烷基链长与活性之间的简单相关性。用其他生物等位基团(硫脲,尿素或(二甲基氨基)甲基)取代胍导致丧失所有测试的活性。因此,发现胍基部分对于这一系列化合物的活性是必不可少的。
  • Furylthiazole derivatives, processes for the preparation thereof and
    申请人:Fujisawa Pharmaceutical Co., Ltd.
    公开号:US05308857A1
    公开(公告)日:1994-05-03
    The invention relates to compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and Q are as described, useful in the treatment of ulcers.
    该发明涉及公式为:##STR1## 其中R.sup.1,R.sup.2,R.sup.3,R.sup.4,A和Q如所述的化合物,对溃疡的治疗有用。
  • KAVAKITA, TAKEHSI;SANO, MITSUXARU;OSUGA, KUNIO;XAGA, KEHJITIRO
    作者:KAVAKITA, TAKEHSI、SANO, MITSUXARU、OSUGA, KUNIO、XAGA, KEHJITIRO
    DOI:——
    日期:——
  • Furylthiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
    申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
    公开号:EP0355612B1
    公开(公告)日:1994-07-27
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