Skip to main content
. 2022 Nov 17;15(11):1427. doi: 10.3390/ph15111427

Table 7.

Compilation of favorable substitutions and SAR for triazole and tetrazole molecules with a traditional azole pharmacophore.

graphic file with name pharmaceuticals-15-01427-i001.jpg
X Y R SAR
Triazole
Inline graphic
F graphic file with name pharmaceuticals-15-01427-i003.jpg 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 graphic file with name pharmaceuticals-15-01427-i004.jpg 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 graphic file with name pharmaceuticals-15-01427-i005.jpg 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 graphic file with name pharmaceuticals-15-01427-i006.jpg 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 graphic file with name pharmaceuticals-15-01427-i007.jpg R1 = Di-chloro-phenyl, furan ring presented promising results against C. albicans
F 1Inline graphic 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
2Inline graphic
F 1Inline graphic 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
2Inline graphic
Tetrazole
Inline graphic
F graphic file with name pharmaceuticals-15-01427-i013.jpg R1 = Alicyclic side chains up to six-members enhance the antifungal potency against C. albicans, C. parapsilosis, C. glabrata, C. neoformans, and A. fumigatus