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

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

Bioorganic & medicinal chemistry letters (2012-10-13)
Suhyun Kim, Sang-Nae Cho, Taegwon Oh, Pilho Kim
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.

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硝酸益康唑, European Pharmacopoeia (EP) Reference Standard
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益康唑, European Pharmacopoeia (EP) Reference Standard
庫存單位
包裝尺寸
供貨能力
價格
數量