title: Synthesis of 1,2,3-triazole derivatives and in vitro antifungal evaluation on Candida strains.
abstract: 1,2,3-Triazoles have been extensively studied as compounds possessing important biological activities. In this work, we describe the synthesis of ten 2-(1-aryl-1H-1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or click chemistry). Next the in vitro antifungal activity of these ten compounds was evaluated using the microdilution broth method against 42 isolates of four different Candida species. Among all tested compounds, the halogen substituted triazole 2-[1-(4-chlorophenyl)-1H-(1,2,3)triazol-4-yl]propan-2-ol, revealed the best antifungal profile, showing that further modifications could be done in the structure to obtain a better drug candidate in the future.
authors.affiliation: Laboratório de Micologia Médica, Centro de Ciências Biológicas, Universidade Federal de Pernambuco-UFPE, 50670-901 Recife, PE, Brazil.
authors.forename: Reginaldo G
authors.initials: RG
authors.lastname: Lima-Neto
authors.forename: Nery N M
authors.initials: NN
authors.lastname: Cavalcante
authors.forename: Rajendra M
authors.initials: RM
authors.lastname: Srivastava
authors.forename: Francisco J B
authors.initials: FJ
authors.lastname: Mendonça Junior
authors.forename: Almir G
authors.initials: AG
authors.lastname: Wanderley
authors.forename: Rejane P
authors.initials: RP
authors.lastname: Neves
authors.forename: Janaína V
authors.initials: JV
authors.lastname: dos Anjos
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001386:Azides / Q000737:chemistry; D002175:Candida / Q000187:drug effects* / Q000254:growth & development; D057930:Click Chemistry; D015195:Drug Design; D008297:Male; D008825:Miconazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D020005:Propanols / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D001386:Azides; D020005:Propanols; D014230:Triazoles; D008825:Miconazole