Ding, Zichao; Ni, Tingjunhong; Xie, Fei; Hao, Yumeng; Yu, Shichong; Chai, Xiaoyun; Jin, Yongsheng; Wang, Ting; Jiang, Yuanying; Zhang, Dazhi published the artcile< Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus>, Electric Literature of 20776-50-5, the main research area is triazole preparation SAR antifungal agent Aspergillus; Antifungal; CYP51; Molecular docking; Synthesis; Triazole.
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, 7-chloro-3-((2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)benzo [d][1,2,3]triazin-4(3H)-one showed comparable antifungal activity against seven pathogenic strains as voriconazole and albaconazole, especially against Aspergillus fumigatus (MIC = 0.25μg/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.
Bioorganic & Medicinal Chemistry Letters published new progress about Aspergillus. 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Electric Literature of 20776-50-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary