Design and synthesis of novel triazole antifungal derivatives by structure-based bioisosterism
The incidence of life-threatening fungal infections is increasing dramatically.In an attempt to develop novel antifungal agents,our previously synthesized pheaoxyalkylpiperazine triazole derivatives were used as lead structures for further optimization,By means of structure-based bioisosterism,triazolone was used as a new bioisostere of oxygen atom.This type of bioisosteric replacement can improve the water solubility without loss of hydrogen-bonding interaction with the target enzyme.A series of triazoione-contaiaing triazoles were rationally designed and synthesized.As compared with fluconazole.several compounds showed higher antifungal activity with broader spectrum,suggesting their potential for further evaluations.
Structure-based bioiso sterism Triazolone Azole Antifungal
Chunquan Sheng Xiaoying Che Wenya Wang Shengzheng Wang Yongbing Cao Zhenyuan Miao Jianzhong Yao Wannian Zhang
School of Pharmacy,Second Military Medical University,325 Guohe Road,Shanghai 200433,Peoples Republic of China
国际会议
南京
英文
176-182
2012-05-13（万方平台首次上网日期，不代表论文的发表时间）