The opportunistic pathogen Candida albicans is the second etiological agent of vaginitis. Candidiasis causes inflammation of the genital tract, which has been associated with complications of pregnancy and increased risks of stillbirth or neonatal death. Also, it is known that 75% of women have at least one vaginal infection caused by this yeast at some point in their lives. Treatment with azoles results in relief of symptoms, but it is only effective in 80%–90% of cases. A clear reflection of many shortcomings of current antifungal therapy includes the limited approved antifungal agents, toxicity and resistance. As part of our efforts to find new anti-Candida agents, we design by bioisosteric replacement and molecular simplification a series of sixteen 2,3-diphenyl-2H-indazole, 3-phenyl-1H-indazole and 1H-pirazole derivatives. The synthesized compounds were tested against two strains of Candida (C. albicans and C. glabrata) using the cylinder-plate method. Compounds showed promising activity in preliminary assays.

Design, synthesis and biological evaluation of new anti-Candida agents

2019 Fall National Meeting

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