Title:
BENZOFURAN, COUMESTANS DERIVATIVES, PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/120210
Kind Code:
A1
Abstract:
The present invention discloses benzofuran and Coumestans derivatives represented by the formulas (I), (II), (III), (IV), a preparation method thereof, and a use of the benzofurans and Coumestans derivative compounds in the treatment of multidrug-resistant tuberculosis diseases. The benzofuran and Coumestans derivatives of the present invention are a type of anti-mycobacterium tuberculosis compound having novel structure and remarkable antibacterial effect, which uses polyketide synthase encoded by the pks13 gene fragment of mycobacterium tuberculosis as target, inhibiting the growth and reproduction of microorganisms, especially inhibiting the synthesis of mycolic acid in the cell wall of mycobacterium tuberculosis. It has potential application prospects in the medicine field.
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Inventors:
YU LIFANG (CN)
ZHANG WEI (CN)
LIU LINGLING (CN)
WANG SHUHUAN (CN)
SHEN DONGHAO (CN)
YANG FAN (CN)
TANG JIE (CN)
BISHAI WILLIAM R (US)
LUN SHICHUN (US)
GUNOSEWOYO HENDRA (AU)
MANSON ABIGAIL L (US)
EARL ASHLEE M (US)
ZHANG WEI (CN)
LIU LINGLING (CN)
WANG SHUHUAN (CN)
SHEN DONGHAO (CN)
YANG FAN (CN)
TANG JIE (CN)
BISHAI WILLIAM R (US)
LUN SHICHUN (US)
GUNOSEWOYO HENDRA (AU)
MANSON ABIGAIL L (US)
EARL ASHLEE M (US)
Application Number:
PCT/CN2018/121968
Publication Date:
June 27, 2019
Filing Date:
December 19, 2018
Export Citation:
Assignee:
UNIV EAST CHINA NORMAL (CN)
UNIV JOHNS HOPKINS (US)
UNIV CURTIN (AU)
UNIV JOHNS HOPKINS (US)
UNIV CURTIN (AU)
International Classes:
C07D307/84; A61K31/4164; A61K31/505; A61P31/06; C07D311/36; C07D493/04
Domestic Patent References:
| WO2016172498A1 | 2016-10-27 | |||
| WO2016112036A1 | 2016-07-14 |
Foreign References:
| FR2269951A1 | 1975-12-05 | |||
| CN104829569A | 2015-08-12 |
Other References:
WEI ZHANG ET AL.: "Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 3, 2 November 2018 (2018-11-02), pages 791 - 803, XP055514827
WAN NAMKUNG: "TMEM16A Inhibitors Reveal TMEM16A as a Minor Component of Calcium-activated Chloride Channel Conductance in Airway and Intestinal Epi- thelial Cells", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 286, no. 3, 21 January 2011 (2011-01-21), pages 2365 - 2374, XP002790464
ZOTOVA, S. A.: "Synthesis and some pharmacological properties of indole and benzofuran derivatives containing an imidazole pharmacophore", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 28, no. 2, 31 December 1994 (1994-12-31), pages 22 - 24
ZOTOVA, S. A.: "Synthesis and pharmacological activity of 2-aryl-3-carbe- thoxy-5-oxybenzofuran derivatives", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 22, 31 December 1988 (1988-12-31), pages 35 - 39
GRINEV, A. N.: "Mannich bases in the series of 5-hydroxybenzofuran de- rivatives", ZHURNAL OBSHCHEI KHIMII, vol. 33, no. 3, 31 December 1963 (1963-12-31), pages 820 - 824
WAN NAMKUNG: "TMEM16A Inhibitors Reveal TMEM16A as a Minor Component of Calcium-activated Chloride Channel Conductance in Airway and Intestinal Epi- thelial Cells", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 286, no. 3, 21 January 2011 (2011-01-21), pages 2365 - 2374, XP002790464
ZOTOVA, S. A.: "Synthesis and some pharmacological properties of indole and benzofuran derivatives containing an imidazole pharmacophore", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 28, no. 2, 31 December 1994 (1994-12-31), pages 22 - 24
ZOTOVA, S. A.: "Synthesis and pharmacological activity of 2-aryl-3-carbe- thoxy-5-oxybenzofuran derivatives", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 22, 31 December 1988 (1988-12-31), pages 35 - 39
GRINEV, A. N.: "Mannich bases in the series of 5-hydroxybenzofuran de- rivatives", ZHURNAL OBSHCHEI KHIMII, vol. 33, no. 3, 31 December 1963 (1963-12-31), pages 820 - 824
Attorney, Agent or Firm:
MSJLAW OFFICE (CN)
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