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.
Anti-Selective Catalytic Asymmetric Nitroaldol Reaction of α-Keto Esters: Intriguing Solvent Effect, Flow Reaction, and Synthesis of Active Pharmaceutical Ingredients
Karasawa, Tomoya,Oriez, Rapha?l,Kumagai, Naoya,Shibasaki, Masakatsu
supporting information, p. 12290 - 12295 (2018/09/27)
A rare-earth metal/alkali metal bimetallic catalyst proved particularly effective for enantioselectively coupling nitroalkanes and α-keto esters in an anti-selective manner to afford synthetically versatile, densely functionalized, and optically active α-nitro tertiary alcohols. A chiral diamide ligand captured two distinct metal cations, giving rise to a catalytically competent solid-phase heterobimetallic catalyst by simple mixing via self-assembly. The advantage of the solid-phase asymmetric catalyst was realized by successful application to the enantio- and diastereoselective reaction in a continuous-flow platform. The use of closely related solvents in terms of structures and polarity parameters, THF and its methylated congener 2-Me-THF, had an unexpectedly large solvent effect both on the reaction rate and the stereoselectivity. The nitroaldol products share a privileged unit for active pharmaceutical ingredients, as demonstrated by the streamlined enantioselective synthesis of the marketed antifungal agents efinaconazole and albaconazole.
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
