Haranahalli, Krupanandan; Lazzarini, Cristina; Sun, Yi; Zambito, Julia; Pathiranage, Senuri; McCarthy, J. Brian; Mallamo, John; Del Poeta, Maurizio; Ojima, Iwao published the artcile< SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents>, Application of C7H4Br2O2, the main research area is antifungal activities SAR Cryptococcus synergistic additive effect fungal strains.
Recently, the fungal sphingolipid glucosylceramide (GlcCer) synthesis has emerged as a highly promising new target for drug discovery of next-generation antifungal agents, and we found two aromatic acylhydrazones as effective inhibitors of GlcCer synthesis based on HTP screening. In the present work, we have designed libraries of new aromatic acylhydrazones, evaluated their antifungal activities (MIC80 and time-kill profile) against C. neoformans, and performed an extensive SAR study, which led to the identification of five promising lead compounds, exhibiting excellent fungicidal activities with very large selectivity index. Moreover, two compounds demonstrated broad spectrum antifungal activity against six other clin. relevant fungal strains. These five lead compounds were examined for their synergism/cooperativity with five clin. drugs against seven fungal strains, and very encouraging results were obtained; e.g., the combination of all five lead compounds with voriconazole exhibited either synergistic or additive effect to all seven fungal strains.
Journal of Medicinal Chemistry published new progress about Cryptococcus neoformans. 603-78-1 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4Br2O2, Application of C7H4Br2O2.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary