Chem. J. Chinese Universities ›› 2014, Vol. 35 ›› Issue (4): 766.doi: 10.7503/cjcu20130688

• Organic Chemistry • Previous Articles     Next Articles

Preliminary Structure-activity Relationship of 2-Ethoxycarbonyl-4-aryl-1,5-benzothiazepines with Antifungal Activity

KANG Wang1, BU Huijuan1, LI Wenhong2, LI Yuan1,*()   

  1. 1. College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang 050024, China
    2. Department of Environment and Chemical Engineering, Hebei College of Industry and Technology, Shijiazhuang 050091, China
  • Received:2013-07-19 Online:2014-04-10 Published:2014-03-06
  • Contact: LI Yuan E-mail:liyuanhbsd@163.com
  • Supported by:
    † Supported by the National Natural Science Foundation of China(No.20972040), the Youth Science Foundation of Hebei Education Department of China(No.Q2012001) and the Youth Science Foundation of Hebei College of Industry and Technology, China(No.Qz1102)

Abstract:

Using 2-ethoxycarbonyl-substituted 1,5-benzothiazepines A1 and A2 as the prototy-pical structure, three series of thirty-four 1,5-benzothiazepine derivatives 11—17 were synthesized and evalu-ated for their antifungal activity against C. neoformans. The results suggested that the ethoxycarbonyl group at the position 2 of benzothiazepines A1 and A2 was essential for their antifungal activity.

Key words: 1,5-Benzothiazepine, Antifungal activity, Structure-activity relationship

CLC Number: 

TrendMD: