Table 7.
X | Y | R | SAR |
---|---|---|---|
Triazole |
F | R1 = Halogens, methyl, cyanide, and nitro groups led to promising antifungal potential against Candida albicans, Candida parapsilosis, Cryptococcus neoformans, and Nannizzia gypsea | |
F or Cl | R1 = Di-chloro-phenyl, paired with Y = Cl, led to the highest antifungal potential of the tested series Y = Cl increased antifungal activity against C. albicans, C. parapsilosis, C. neoformans, Epidermophyton floccosum and Trichophyton mentagrophytes |
||
F | R1 = butyrate and butyric acid increased antifungal potential against all tested strains; 4-acetyl or 4-trifluoromethoxy-phenyl groups increased activity for C. albicans; 2-methyl-phenyl group increased activity against C. parapsilosis and Candida glabrata | ||
F or Cl | R1 = 4-Chloro showed high antifungal activity against C. albicans, C. glabrata, C. parapsilosis, Candida krusei and Candida tropicalis. Y = F analogs presented higher antifungal potency |
||
F | R1 = Di-chloro-phenyl, furan ring presented promising results against C. albicans | ||
F | 1 | 1: R1 = alkyl chains were not beneficial for antifungal activity 2: R1–3 = one fluor substituent; two chlorine substituents: increased antifungal activity against C. albicans |
|
2 | |||
F | 1 | 1 and 2: positional isomers R1 = trifluoromethyl led to high antifungal activity against C. albicans, C. tropicalis, C. parapsilosis, C. krusei, C. glabrata, C. neoformans, Aspergillus fumigatus, and Aspergillus niger |
|
2 | |||
Tetrazole |
F | R1 = Alicyclic side chains up to six-members enhance the antifungal potency against C. albicans, C. parapsilosis, C. glabrata, C. neoformans, and A. fumigatus |