Design, Synthesis and Anticandidal Evaluation of Indazole and Pyrazole Derivatives
Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search...
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Veröffentlicht in: | Pharmaceuticals (Basel, Switzerland) Switzerland), 2021-02, Vol.14 (3), p.176 |
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Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search for new candicidal compounds is certainly a priority. In this regard, a series of indazole and pyrazole derivatives were designed in this work, employing bioisosteric replacement, homologation, and molecular simplification as new anticandidal agents. Compounds were synthesized and evaluated against
,
, and
strains. The series of 3-phenyl-1
-indazole moiety (
) demonstrated to have the best broad anticandidal activity. Particularly, compound
, with
,
-diethylcarboxamide substituent, was the most active against
and both miconazole susceptible and resistant
species. Therefore, the 3-phenyl-1
-indazole scaffold represents an opportunity for the development of new anticandidal agents with a new chemotype. |
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ISSN: | 1424-8247 1424-8247 |
DOI: | 10.3390/ph14030176 |