留言板

尊敬的读者、作者、审稿人, 关于本刊的投稿、审稿、编辑和出版的任何问题, 您可以本页添加留言。我们将尽快给您答复。谢谢您的支持!

姓名
邮箱
手机号码
标题
留言内容
验证码
x 关闭 永久关闭

应中央军委要求，2022年9月起，《药学实践杂志》将更名为《药学实践与服务》，双月刊，正文96页；2023年1月起，拟出版月刊，正文64页，数据库收录情况与原《药学实践杂志》相同。欢迎作者踊跃投稿！

2-位取代苯并呋喃类化合物的生物活性及合成研究进展

陈焕,  李科

downloadPDF
文章导航 > 药学实践与服务  > 2013 >  31(1): 5-10,71
陈焕, 李科. 2-位取代苯并呋喃类化合物的生物活性及合成研究进展[J]. 药学实践与服务, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
引用本文: 陈焕, 李科. 2-位取代苯并呋喃类化合物的生物活性及合成研究进展[J]. 药学实践与服务, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
shu
CHEN Huan, LI Ke. Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
Citation: CHEN Huan, LI Ke. Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
shu

2-位取代苯并呋喃类化合物的生物活性及合成研究进展

doi: 10.3969/j.issn.1006-0111.2013.01.002

  • 第二军医大学药学院药物化学教研室, 上海 200433

Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives

  • Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • 摘要: 苯并呋喃衍生物是当前研究杂环芳香族化合物的热点之一。据文献报道该类化合物具有抗肿瘤,抗氧化,钙内流阻滞,血管紧张素II受体拮抗,腺苷A1受体拮抗,抗真菌、抗菌活性和血小板聚集拮抗等药理作用。由于苯并呋喃具有广泛活性,因此吸引很多学者对其进行研究。为了更好地研究该类化合物的合成和生物活性,本文对近几年来文献报道的具有良好生物活性的2-位取代苯并呋喃衍生物进行综述,并对它们的合成方法进行概括,为开发新型2-取代苯并呋喃类化合物提供参考。
    Abstract: Benzofuran derivatives were a series of attracting heterocyclic compounds with a variety of biological activity. Based on the recently published literatures, these derivatives had shown antitumor, antioxidant, calcium influx blockade, angiotensin II receptor antagonistic, adenosine A1 receptor antagonistic, antifungal, antibacterial and platelet aggregation antagonistic activities. As Benzofuran derivatives had broad activity, which had attracted many research interests. In order to better study of these compounds both in synthesis and biological activity, the review focused on the biological activity and synthetic methods of 2-substituted Benzofuran derivatives in recent years, which would provide valuable information for the development of 2-substituted benzofuran compounds.
  • [1] Katritzky AR, Rees CW, Scriven EF, et al. Comprehensive Heterocyclic Chemistry II[M]. Oxford:Pergamon Press, 1996: 167.
    [2] Fikret K, Murat K, Haki K, et al. Synthesis and oxidant properties of novel (5-bromobenzofuran-2-yl)(3-methyl-3-mesitylcyclobutyl)ketonethiosemicarbazone[J]. Eur J Med Chem, 2006, 41(5): 664.
    [3] Cumhur K, Misir A, Murat K.Synthesis and antimicrobial activity of some novel derivatives of benzofuran: Part 2. The synthesis and antimicrobial activity of some novel 1-(1-benzofuran-2-yl)-2-mesitylethanone derivatives[J]. Eur J Med Chem, 2008, 43(8): 300.
    [4] Bakr F,Abdel W, Hatem A,et al. Synthesis and antimicrobial evaluation of 1-(benzofuran-2-yl)-4-nitro-3-arylbutan-1-ones and 3-(benzofuran-2-yl)-4,5-dihydro-5-aryl-1-[4-(aryl)-1,3-thiazol-2-yl]-1H-pyrazoles[J]. Eur J Med Chem, 2009, 44(16): 2632.
    [5] Stephane P, Sook WY, Martyn J, et al. Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles][J]. Bioorg Med Chem, 2006, 14(11): 3643.
    [6] Jerzy K, Kinga O, Irena W, et al. Synthesis and structural characterization of derivatives of 2-and 3-benzo[b]furan carboxylic acids with potential cytotoxic activity[J]. IL FARMACO, 2005, 60(6-7): 519.
    [7] Romeo R, Pier G, Taradas S,et al. Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization[J]. Bioorg Med Chem, 2008, 16(18): 8419.
    [8] Pierre YM, Jennifer DA, Timothy AG, et al. Design, synthesis and structure-activity relationship of novel RXR-selective modulators[J]. Bioorg Med Chem Lett, 2004, 14(6): 1593.
    [9] Masahiro I, Shingo N, Shingo Y,et al. Discovery of a new chemical lead for a matrix metalloproteinase inhibitor[J]. Bioorg Med Chem, 2006, 14(12): 4241.
    [10] Siavosh M, Andrea U, Christophe C,et al. Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones[J]. Bioorg Med Chem, 2007, 15(5): 187.
    [11] Manish D, Brajendra K, Akhilesh K,et al. Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors[J]. Bioorg Med Chem, 2007, 15(2): 727.
    [12] Kuntal M, Yadvendra K, Agrawa D,et al. Synthesis, and antitubercular evaluation of novel series benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs[J]. Eur J Med Chem, 2010, 10(9): 1016.
    [13] Kham MW, Alam MJ, Rashid MA,et al. A new structural alternative in benzo[b]furans for antimicrobial activity[J]. Bioorg Med Che, 2005, 13(16): 4796.
    [14] Bernd P, Sonja B, Rolf H,et al. Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor[J]. Bioorg Med Chem Lett, 2006, 16(12): 3162.
    [15] Jung WH, Da HC, Jae H,et al. Facile Preparation of 2-Arylbenzo[b]furan Molecules and Their Antiinflammatory Effects[J]. Bull Korean Chem Soc, 2010, 31(4): 4965.
    [16] Michael CW, Dawn T, Adam TG,et al. Palladium-catalysed intramolecular enolate O-arylation and thio-enolate S-arylation: synthesis of benzo[b]furans and benzo[b]thiophenes[J]. Tetrahedron,2006, 62(49): 11513.
    [17] Sanjay SP, Vijaykumar S, More KV,et al. Ultrasound promoted copper-, ligand-and amine-free synthesis of benzo [b]furans/nitro benzo[b]furans via Sonogashira coupling-5-endo-dig-cyclization[J]. Ultrason Sonochem, 2008, 15(5): 853.
    [18] Antonella B, Lucia C, Maria F,et al. Effcient synthesis of 5-nitro-benzo[b]furans via 2-bromo-4-nitro-phenyl acetates[J]. Tetrahedron Lett, 2010, 51(21): 2824.
    [19] Hu J, Wang XC, Guo LN,et al. Pd/C-catalyzed cyclization/isomerization: A new route to 2-aroyl-3-vinyl benzo[b]furans via carbon-carbon bond formation[J]. Catal Commun, 2010, 11(5): 346.
    [20] Pei LX,Li YM,Bu XI,et al. One-pot synthesis of 5.6-dihydroxylated benzo[b]furan derivatives[J]. Tetrahedron Lett, 2006, 47(15): 2615.
    [21] Li HF,Liu J,Yan B,et al. Newdomino approach for the synthesis of 2,3-disubstituted benzo[b]furans via copper-catalyzed multi-component coupling reactions followed by cyclization[J]. Tetrahedron Lett, 2009, 50(20): 2353.
  • [1] 毛智毅, 王筱燕, 陈晓颖, 汤逸斐.  度拉糖肽联合二甲双胍对肥胖型2型糖尿病患者机体代谢、体脂成分及血清脂肪因子的影响 . 药学实践与服务, 2024, 42(7): 305-309. doi: 10.12206/j.issn.2097-2024.202305032
    [2] 桂明珠, 李静, 李志玲.  儿童伏立康唑的血药浓度与CYP2C19、CYP2C9和CYP3A5基因多态性的相关性研究 . 药学实践与服务, 2024, 42(): 1-5. doi: 10.12206/j.issn.2097-2024.202402020
    [3] 陈静, 何瑞华, 翁月, 徐熠, 刘静, 黄瑾.  基于网络药理学和分子对接技术探究定清片活性成分治疗白血病的作用机制 . 药学实践与服务, 2024, 42(11): 479-486. doi: 10.12206/j.issn.2097-2024.202401073
    [4] 陈炳辰, 王思真, 郭贝贝, 杨峰.  紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究 . 药学实践与服务, 2024, 42(9): 379-384, 410. doi: 10.12206/j.issn.2097-2024.202404062
    [5] 顾佳钰, 胡馨儿, 王晓飞, 张颖, 张海, 曹岩.  侧流免疫层析定量检测方法的研究进展 . 药学实践与服务, 2024, 42(7): 273-277, 284. doi: 10.12206/j.issn.2097-2024.202307037
    [6] 景凯, 杨慈荣, 张圳, 臧艺蓓, 刘霞.  黄芪甲苷衍生物治疗慢性心力衰竭小鼠的药效评价及作用机制研究 . 药学实践与服务, 2024, 42(5): 190-197. doi: 10.12206/j.issn.2097-2024.202310004
    [7] 赖立勇, 夏天爽, 徐圣焱, 蒋益萍, 岳小强, 辛海量.  中药青蒿抗氧化活性的谱效关系研究 . 药学实践与服务, 2024, 42(5): 203-210, 216. doi: 10.12206/j.issn.2097-2024.202211012
  • 加载中
WeChat 点击查看大图
计量
  • 文章访问数:  4563
  • HTML全文浏览量:  375
  • PDF下载量:  231
  • 被引次数: 0
出版历程
  • 收稿日期:  2011-03-14
  • 修回日期:  2012-06-10

2-位取代苯并呋喃类化合物的生物活性及合成研究进展

doi: 10.3969/j.issn.1006-0111.2013.01.002
  • 第二军医大学药学院药物化学教研室, 上海 200433
  • 收稿日期: 2011-03-14
  • 修回日期: 2012-06-10

摘要: 苯并呋喃衍生物是当前研究杂环芳香族化合物的热点之一。据文献报道该类化合物具有抗肿瘤,抗氧化,钙内流阻滞,血管紧张素II受体拮抗,腺苷A1受体拮抗,抗真菌、抗菌活性和血小板聚集拮抗等药理作用。由于苯并呋喃具有广泛活性,因此吸引很多学者对其进行研究。为了更好地研究该类化合物的合成和生物活性,本文对近几年来文献报道的具有良好生物活性的2-位取代苯并呋喃衍生物进行综述,并对它们的合成方法进行概括,为开发新型2-取代苯并呋喃类化合物提供参考。

English Abstract

陈焕, 李科. 2-位取代苯并呋喃类化合物的生物活性及合成研究进展[J]. 药学实践与服务, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
引用本文: 陈焕, 李科. 2-位取代苯并呋喃类化合物的生物活性及合成研究进展[J]. 药学实践与服务, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
shu
CHEN Huan, LI Ke. Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
Citation: CHEN Huan, LI Ke. Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
shu

    全文HTML

参考文献 (21)

目录

    /

    返回文章
    返回

    版权所有：《药学实践与服务》编辑委员会

    主管、主办: 中国人民解放军海军军医大学地址: 上海市杨浦区国和路325号邮政编码: 200433

    电话: （021）81871324,81871397 E-mail: yxsjzzs@163.com

    网站备案号 沪ICP备05003363号-1

    本系统由 北京仁和汇智信息技术有限公司 开发    百度统计