206350-07-4Relevant articles and documents
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus
Ding, Zichao,Ni, Tingjunhong,Xie, Fei,Hao, Yumeng,Yu, Shichong,Chai, Xiaoyun,Jin, Yongsheng,Wang, Ting,Jiang, Yuanying,Zhang, Dazhi
, (2020/01/13)
The incidence of invasive fungal infections has dramatically increased for several decades. In order to discover novel antifungal agents with broad spectrum and anti-Aspergillus efficacy, a series of novel triazole derivatives containing 1,2,3-benzotriazin-4-one was designed and synthesized. Most of the compounds exhibited stronger in vitro antifungal activities against tested fungi than fluconazole. Moreover, 6m showed comparable antifungal activity against seven pathogenic strains as voriconazole and albaconazole, especially against Aspergillus fumigatus (MIC = 0.25 μg/ml), and displayed moderate antifungal activity against fluconazole-resistant strains of Candida albicans. A clear SAR study indicated that compounds with groups at the 7-position resulted in novel antifungal triazoles with more effectiveness and a broader-spectrum.
New azole antifungals. 3. Synthesis and antifungal activity of 3- substituted-4(3H)-quinazolinones
Bartroli, Javier,Turmo, Enric,Algueró, Mònica,Boncompte, Eulàlia,Vericat, Maria L.,Conte, Lourdes,Ramis, Joaquim,Merlos, Manuel,García-Rafanell, Julián,Forn, Javier
, p. 1869 - 1882 (2007/10/03)
A series of azole antifungal agents featuring a quinazolinone nucleus have been subjected to studies of structure - activity relationships. In general, these compounds displayed higher in vitro activities against filamentous fungi and shorter half-lives t