47545-72-2Relevant academic research and scientific papers
Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease
Lu, Xin,He, Si-yu,Li, Qi,Yang, Hongyu,Jiang, Xueyang,Lin, Hongzhi,Chen, Yao,Qu, Wei,Feng, Feng,Bian, Yaoyao,Zhou, You,Sun, Haopeng
, p. 1665 - 1674 (2018/02/23)
In our endeavor towards the development of potent multi-target ligands for the treatment of Alzheimer's disease, miconazole was identified to show BuChE-IDO1 dual-target inhibitory effects. Morris water maze test indicated that miconazole obviously ameliorated the cognitive function impaired by scopolamine. Furthermore, it showed good safety in primary hepatotoxicity evaluation. Based on these results, we designed, synthesized, and evaluated a series of miconazole derivatives as BuChE-IDO1 dual-target inhibitors. Out of the 12 compounds, 5i and 5j exhibited the best potency in enzymatic evaluation, thus were selected for subsequent behavioral study, in which the two compounds exerted much improved effect than tacrine. Meanwhile, 5i and 5j displayed no apparent hepatotoxicity. The results suggest that miconazole analogue offers an attractive starting point for further development of new BuChE-IDO1 dual-target inhibitors against Alzheimer's disease.
A new series of miconazole analogs: Synthesis and in vitro antifungal and antimycobacterial activities
Fioravanti, Rossella,Biava, Mariangela,Porretta, Giulio Cesare,Lampis, Giorgio,Deidda, Delia,Pompei, Raffaello
, p. 162 - 175 (2007/10/03)
The synthesis and antimicrobial activity of new miconazole analogs are reported. All compounds showed good antimycobacterial activity; some of them were also active against some strains of Candida albicans and Candida sp.. Of the synthesized compounds, two showed good activity both against some strains of Mycobacterium and some strains of Candida. Structure-activity relationships are discussed.
