Design and synthesis of 1H-1,2,3-triazoles derived from econazole as antitubercular agents

Suhyun Kim, Sang Nae Cho, Taegwon Oh, Pilho Kim

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47 Citations (Scopus)


Econazole has been known to be active against Mycobacterium tuberculosis. We have designed and synthesized 1H-1,2,3-triazoles derived from econazole as antitubercular agents. The majority of triazole derivatives have been prepared by microwave-assisted click chemistry. It turned out that all of the prepared triazoles had no antifungal activities. However, most of the hydroxy-triazoles (6a and 10) apparently turned out to have antitubercular activities. Overall, hydroxy-triazoles 10 were more active than their corresponding ether-triazoles 11. While the MIC value of hydroxy-triazole 10d was as good as econazole (16 μg/mL), the MIC value of 10a was two-fold more active than econazole, suggesting that this 1H-1,2,3-triazole scaffold (3) could be further optimized to develop Mtb specific agents.

Original languageEnglish
Pages (from-to)6844-6847
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number22
Publication statusPublished - 2012 Nov 15

Bibliographical note

Funding Information:
This work was supported by Korea Research Institute of Chemical Technology (KRICT) and by the International Research & Development Program of the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (MEST) of Korea (Grant number: K20501000001-09E0100-00110, FY 2009)

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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