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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

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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.
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    [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.
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    [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.
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    [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.
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    [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.
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    [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.
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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

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