首页|SYNTHESIS AND BIOLOGICAL ACTIVITIES OF DIOSGENIN-TRIAZOLE CONJUGATES WITH A 1,3-DIPOLAR CYCLOADDITION REACTION

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF DIOSGENIN-TRIAZOLE CONJUGATES WITH A 1,3-DIPOLAR CYCLOADDITION REACTION

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A novel series of diosgenin-triazole conjugates(10a-d,11a-c,12a-c,13a-c)was designed and synthesized as antifungal agents by using a 1,3-dipolar cycloaddition reaction in the presence of Cu(I)catalyst.All the title compounds were characterized by ~1H NMR,~(13)C NMR,and Q-TOF-MS.Results of preliminary antifungal tests against seven human pathogenic fungi in vitro revealed that half of the target compounds exhibited moderate or even better antifungal activities against Candida albicans Y0109 and C.albicans SC5314 species.Compound lOd showed excellent antifungal activities toward C.albicans Y0109 and C.albicans SC5314 than itraconazole,with MIC_(80)value of 1 μg/mL,respectively.

triazolefluconazolesapogenindiosgeninconjugatesantifungal activity

Jun Liao、Guochao Liao、Yun Gao

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Department of Biochemistry and Molecular Biology,College of Basic Medical Sciences,Second Military Medical University,200433,Shanghai,R R.China

International Institute for Translational Chinese Medicine,Guangzhou University of Chinese Medicine,510006,Guangzhou,P.R.China

2021

Химия природных соединений

Химия природных соединений

ISSN:0023-1150
年,卷(期):2021.(6)