Bioorganic & Medicinal Chemistry Letters 2012-11-15

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

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

文献索引：Bioorg. Med. Chem. Lett. 22(22) , 6844-7, (2012)

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摘要

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.Copyright © 2012 Elsevier Ltd. All rights reserved.