A series of novel ethyl-7-（（1-（benzyl）-1H-1,2,3-triazol-4-yl）methoxy）-2-oxo-2H-chromene-3-carboxylates 8a-h as potential antifungal agents were synthesized via click chemistry. The antifungal activity was evalua...A series of novel ethyl-7-（（1-（benzyl）-1H-1,2,3-triazol-4-yl）methoxy）-2-oxo-2H-chromene-3-carboxylates 8a-h as potential antifungal agents were synthesized via click chemistry. The antifungal activity was evaluated against five human pathogenic fungal strains, such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger and Cryptococcus neoformans. Compound 8c, 8d, 8e and 8h were found to be equipotent against C. albicans when compared with miconazole and compound 8f was found to be two-fold more active compared with miconazole and equipotent to fluconazole against C.albicans. The coumarin-based triazole derivatives were also evaluated for antioxidant activity and compound 8a was found to be potent antioxidant when compared with standard drug. Furthermore,molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C. albicans enzyme P450 cytochrome lanosterol 14 ademethylase. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug candidates.展开更多
A small focused library of eighteen new 1,2,3-triazole tethered acetophenones has been efficiently prepared via click chemistry approach and evaluated for their antifungal and antioxidant activity.The antifungal activ...A small focused library of eighteen new 1,2,3-triazole tethered acetophenones has been efficiently prepared via click chemistry approach and evaluated for their antifungal and antioxidant activity.The antifungal activity was evaluated against five human pathogenic fungal strains：Candida albicans,Fusarium oxysporum,Aspergillus flavus,Aspergillus niger,and Cryptococcus neoformans.Among the synthesized compounds,9c,9i,and 9p found to be more potent antifungal agents that the reference standard.These 1,2,3-triazole based derivatives were also evaluated for antioxidant activity,and compound 9h was found to be the most potent antioxidant as compared to the standard drug.Furthermore,molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C.albicans enzyme P450 cytochrome lanosterol14oi-demethylase.Moreover,the synthesized compounds were also analyzed for ADME properties and showed potential as good oral drug candidates.展开更多
文摘A series of novel ethyl-7-（（1-（benzyl）-1H-1,2,3-triazol-4-yl）methoxy）-2-oxo-2H-chromene-3-carboxylates 8a-h as potential antifungal agents were synthesized via click chemistry. The antifungal activity was evaluated against five human pathogenic fungal strains, such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger and Cryptococcus neoformans. Compound 8c, 8d, 8e and 8h were found to be equipotent against C. albicans when compared with miconazole and compound 8f was found to be two-fold more active compared with miconazole and equipotent to fluconazole against C.albicans. The coumarin-based triazole derivatives were also evaluated for antioxidant activity and compound 8a was found to be potent antioxidant when compared with standard drug. Furthermore,molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C. albicans enzyme P450 cytochrome lanosterol 14 ademethylase. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug candidates.
基金the University Grant Commission-Department of Science and Technology New Delhi for financial support under UGC-SAP and DST-FIST schemes
文摘A small focused library of eighteen new 1,2,3-triazole tethered acetophenones has been efficiently prepared via click chemistry approach and evaluated for their antifungal and antioxidant activity.The antifungal activity was evaluated against five human pathogenic fungal strains：Candida albicans,Fusarium oxysporum,Aspergillus flavus,Aspergillus niger,and Cryptococcus neoformans.Among the synthesized compounds,9c,9i,and 9p found to be more potent antifungal agents that the reference standard.These 1,2,3-triazole based derivatives were also evaluated for antioxidant activity,and compound 9h was found to be the most potent antioxidant as compared to the standard drug.Furthermore,molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C.albicans enzyme P450 cytochrome lanosterol14oi-demethylase.Moreover,the synthesized compounds were also analyzed for ADME properties and showed potential as good oral drug candidates.
