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Synthesis and Biological Activity of Flavane Derivatives
  • ISSN号:1001-604X
  • 期刊名称:《中国化学:英文版》
  • 时间:0
  • 分类:R978[医药卫生—药品;医药卫生—药学] R914.5[医药卫生—药物化学;医药卫生—药学]
  • 作者机构:[1]Department of Chemistry, Beijing Normal University, Beijing 100875, China, [2]Protection and Utilization of Chinese Medicine Resources of Beijing Key Laboratory, Beifing Normal University, Beijing 100875, China, [3]State Key Laboratory of Pharmaceutical Biotechnology, Institute of Functional Biomolecules, Nanjing University, Nanfing, Jiangsu 210093, China
  • 相关基金:Project supported by the Key Project of the Ministry of Education of China (No. 03013), the National Natural Science Foundation of China (No. 20372010) and Trans-century Training Program Foundation for the Talents, Ministry of Education of China and Chinese Academy of Medical Sciences.
中文摘要:

当钥匙走,一条有效、可行的合成途径与 chalcones 和随后的环合的减小从代替的 benzaldehyde 为一连串的新 flavane 衍生物的合成被开发。产品的纯净和结构被元素的分析和它的红外, 1H 和 13C NMR,和集体系列的联合证实。这些合成混合物为黄质 oxidase (XO ) 被测试对 Candida albicans 的抑制和抗真菌的行动, Cryptococcus neoformans,曲霉属菌 sp。并且 Trichophyton rubrum。7-Hydrazinocarbonylmethoxy-4-methoxyflavane (9 ) 与 IC50=76.4 mol/L,和抗真菌的化合物是的大多数有势力被发现是大多数 XO 禁止有对 Trichophyton rubrum 的最小的抑制集中 MIC8 g/mL 的 4-hydrazinocarbonylmethoxyflavane (12 ) 。

英文摘要:

An efficient and feasible synthetic approach was developed for the synthesis of an array of new flavane derivafives from the substituted benzaldehyde with the reduction of chalcones and subsequent cyclization as the key steps. The purity and structure of the products were confirmed by the elemental analysis and a combination of its IR, ^1H and ^13C NMR, and mass spectra. These synthetic compounds were tested for xanthine oxidase (XO) inhibitions and antifungal actions against Candida albicans, Cryptococcus neoformans, Aspergillus sp. and Trichophyton rubrum. 7-Hydrazinocarbonylmethoxy-4'-methoxyflavane (9) was found to be the most XO inhibitory with IC50=76.4 μmol/L, and the most potent antifungal compound was 4'-hydrazinocarbonylmethoxyflavane (12) with minimal inhibition concentration MIC=8 μg/mL against Trichophyton rubrum.

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期刊信息
  • 《中国化学:英文版》
  • 主管单位:
  • 主办单位:中国化学会
  • 主编:
  • 地址:上海市枫林路354号中科院上海有机化学研究所
  • 邮编:200032
  • 邮箱:
  • 电话:021-54925243
  • 国际标准刊号:ISSN:1001-604X
  • 国内统一刊号:ISSN:31-1547/O6
  • 邮发代号:4-646
  • 获奖情况:
  • 中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国化学文摘(网络版),荷兰文摘与引文数据库,美国科学引文索引(扩展库),日本日本科学技术振兴机构数据库,英国英国皇家化学学会文摘
  • 被引量:175