114729-71-4Relevant academic research and scientific papers
Improved potency and reduced toxicity of the antifungal peptoid AEC5 through submonomer modification
Middleton, Madyson P.,Armstrong, Scott A.,Bicker, Kevin L.
, p. 3514 - 3519 (2018)
As proteolytically stable peptidomimetics, peptoids could serve as antifungal agents to supplement a therapeutic field wrought with toxicity issues. We report the improvement of an antifungal peptoid, AEC5, through an iterative structure-activity relationship study. A sarcosine scan was used to first identify the most pharmacophorically important peptoid building blocks of AEC5, followed by sequential optimization of each building block. The optimized antifungal peptoid from this study, β-5, has improved potency towards Cryptococcus neoformans and decreased toxicity towards mammalian cells. For example, the selectivity ratio for C. neoformans over mammalian fibroblasts was improved from 8 for AEC5 to 37 for β-5.
ANTIFUNGAL PEPTOIDS
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Paragraph 0079, (2020/07/07)
Described herein are antifungal peptoids, the development and characterization of the antifungal peptoids, methods of making the antifungal peptoids, and methods of using the antifungal peptoids. In some embodiments, the antifungal peptoids may be administered to a subject infected with or at risk of being infected with pathogenic fungi including, for example Cryptococcus spp. In some embodiments, the Cryptococcus spp. may include C. neoformans or C. gattii or both.
Synthesis and anti-HIV-1 integrase activity of modified dinucleotides
Aubert, Yves,Chassignol, Marcel,Roig, Victoria,Mbemba, Gladys,Weiss, Julien,Meudal, Herve,Mouscadet, Jean-Francois,Asseline, Ulysse
experimental part, p. 5029 - 5044 (2010/01/16)
The synthesis of a series of thirty-eight new modified dinucleotides and dinucleotide conjugate analogues of d-5′ApC3′ is described. The inhibitory activity of these compounds toward HIV-1 integrase was examined in enzymatic assays using the natural dinucleotide as a reference. Among the compounds, a perylene-dinucleotide conjugate has shown a two micromolar anti-integrase activity due to the presence of both the intercalator and the dinucleotide.
