Synthesis and Antifungal Activity of New 2-[(z)-1-(3,5-diaryl-1,3,4-thiadiazol-2(3h)-ylidene)methyl]-3,5-diaryl-1,3,4-thiadiazol-3-ium Chlorides

Quantification of a New Antifungal Drug Based on 1,3,4-Thiadiazole by HPLC-ESI/MS: Method Development, Validation and Pharmacokinetic Application

“…2-[(Z)-1-(3,5-diphenyl-1,3,4-thiadiazol-2(3H)-ylidene)methyl]-3,5-diphenyl-1,3,4-thiadiazol-3-ium chloride (TDZ, pharmaceutical substance, 99.5 % [18], trifluoroacetic acid (TFA, purity grade 99.0 %, Merck, USA), HPLC-grade acetonitrile (Panreac, Germany), deionized water for HPLC was prepared by Arium mini (Sartorius, Germany), sample solvent -solution of acetonitrile and 0.03 % TFA (1:1, v/v), filter-nylon i.d. 0.45 μm (Sartorius, Germany).…”

“…1,3,4-Thiadiazoles constitute an important class of biologically active compounds with a wide variety of pharmacological applications including antitumor [1,2], antimicrobial [3][4][5][6][7], anti-tuberculosis [8], antioxidant [9], antiviral [10], anti-inflammatory [11][12][13] and antifungal [14][15][16][17] activities. Antifungal activity was found for a new heterocyclic compound [(Z)-1-(3,5-diphenyl-1,3,4-thiadiazol-2(3H)-ylidene)-methyl]-3,5-diphenyl-1,3,4-thiadiazol-3-ium chloride (TDZ) [18]. The authors [18,19] have established that the minimum inhibitory concentration (MIC) of TDZ against C. tropicalis was 1 μg mL − 1 , against Aspergillus niger − 16 μg mL − 1 , against Mucor racemosus − 32 μg mL − 1 and against Rhizopus nigricans − 250 μg mL − 1 .…”

“…Antifungal activity was found for a new heterocyclic compound [(Z)-1-(3,5-diphenyl-1,3,4-thiadiazol-2(3H)-ylidene)-methyl]-3,5-diphenyl-1,3,4-thiadiazol-3-ium chloride (TDZ) [18]. The authors [18,19] have established that the minimum inhibitory concentration (MIC) of TDZ against C. tropicalis was 1 μg mL − 1 , against Aspergillus niger − 16 μg mL − 1 , against Mucor racemosus − 32 μg mL − 1 and against Rhizopus nigricans − 250 μg mL − 1 . Voriconazole and caspofungin having antifungal activity against Candida yeasts were used as reference drugs, and their antifungal activities were worse than antifungal activity of TDZ against all listed yeasts.…”