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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
ABSTRAKT

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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Econazole, European Pharmacopoeia (EP) Reference Standard
SKU
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Econazole nitrate, European Pharmacopoeia (EP) Reference Standard
SKU
Gabaryty przesyłki
Dostępność
Cena netto
Ilość