2014
DOI: 10.1021/cr5003134
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Drug Strategies Targeting CYP51 in Neglected Tropical Diseases

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Cited by 83 publications
(60 citation statements)
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“…6 Several new targets are the subject of ongoing research for the development of anti-Chagas agents. 7,8 Cruzain, a critical cysteine protease of T. cruzi, is a drug target for Chagas disease. 9 Efficacy of the vinyl sulfone inhibitors K-11777 (1) and WRR-483 (2) ( Figure 1) against cruzain in mouse 10,11 and dog 12 models of Chagas' disease have been demonstrated.…”
mentioning
confidence: 99%
“…6 Several new targets are the subject of ongoing research for the development of anti-Chagas agents. 7,8 Cruzain, a critical cysteine protease of T. cruzi, is a drug target for Chagas disease. 9 Efficacy of the vinyl sulfone inhibitors K-11777 (1) and WRR-483 (2) ( Figure 1) against cruzain in mouse 10,11 and dog 12 models of Chagas' disease have been demonstrated.…”
mentioning
confidence: 99%
“…[10][11][12] If their activities are inhibited, the synthesis of ergosterol will be blocked, some upstream components and intermediates (such as 14a-methyl sterol) accumulate in the fungal cell, and eventually cause the death of the fungi. 13,14 Currently, conventional antifungal agents can be divided into two categories based on the mode of action of the blocking ergosterol, including SE inhibitors (e.g., nai-ne, terbinane and liranaate), and CYP51 inhibitors (e.g., miconazole, itraconazole and uconazole), many of them have been developed for many years, and show good therapeutic effects in the clinic. [15][16][17] However, the two kinds of inhibitors have their shortcomings, such as a narrow antimicrobial spectrum, drug resistance and low bioavailability, which negatively affect their clinical efficacy.…”
Section: Introductionmentioning
confidence: 99%
“…Quinoline clubbed with pyrazole has been reported for antibacterial, antifungal, antitubercular, anticancer, activities. Pyrazolyl‐triazole were reported for antibacterial, antifungal, and anticancer activities. Quinoline‐triazole compounds were reported for antimicrobial antitubercular and antimalarial activities.…”
Section: Introductionmentioning
confidence: 99%