Synthesis and Antifungal Activity of Novel Triazole Compounds Containing Piperazine Moiety
Yanwei Wang,
Kehan Xu,
Guojing Bai,
Lei Huang,
Qiuye Wu,
Weihua Pan,
Shichong Yu
Affiliations
Yanwei Wang
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Kehan Xu
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Guojing Bai
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Lei Huang
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Qiuye Wu
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Weihua Pan
Shanghai Key Laboratory of Molecular Medical Mycology, Department of Dermatology, Shanghai Changzheng Hospital, Second Military Medical University, 415 Fengyang Road, Shanghai 200003, China
Shichong Yu
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325Guohe Road, Shanghai 200433, China
Design and synthesis of triazole library antifungal agents having piperazine side chains, analogues to fluconazole were documented. The synthesis highlighted utilization of the click chemistry on the basis of the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by 1H-NMR, 13C-NMR, MS and IR. The influences of piperazine moiety on in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi.
