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Medicinal Chemistry Research

, Volume 26, Issue 10, pp 2491–2498 | Cite as

Synthesis and bioactivity evaluation of novel azoles containing dithiocarbamate moieties

  • Ben  Fu
  • Maocheng Wu
  • Lu Huang
  • Qiuye Wu
  • Shudong Wang
  • Xiaoyun Chai
Original Research
  • 92 Downloads

Abstract

A series of novel azoles, N-methyl-N-[2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)]-propyl-(1-substituted phenyl)-dithiocarbamate has been designed, synthesized, and screened for antifungal activity by minimum inhibitory concentration. Results of preliminary antifungal tests showed that most of the title compounds had good antifungal activities against nearly all the tested fungal pathogens, especially against the Candida species. The most surprising finding of this study is that compound 4a, 4e, and 4k exhibited higher activities than fluconazole against Aspergillus fumigatus.

Keywords

Azole Synthesis Antifungal activity CACYP51 

Notes

Acknowledgements

This work was supported by the National Natural Science Foundation of China (Nos. 20972188), a Grant from Science & Technology Commission of Shanghai (Nos. 09dZ1976700), and by Shanghai Leading Academic Discipline Project Number: B906.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  1. 1.Department of Organic Chemistry, School of PharmacySecond Military Medical UniversityShanghaiChina
  2. 2.Department of PharmaceuticalNanjing General Hospital of Nanjing Military CommandNanjingChina

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