A New and Efficient Epoxide Ring Opening via Poor Nucleophiles: Indole, p‐Nitroaniline, Borane and O‐Trimethylsilylhydroxylamine in Lithium Perchlorate.

Heydari, Akbar; Mehrdad, Morteza; Maleki, Aziz; Ahmadi, Nafiseh

doi:10.1002/chin.200445040

Cited by 2 publications

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“…Acylation and sulfonylation of 44 provided compounds 52 and 53 . N -Phenyl analogue 57 was obtained in four steps starting from 2-methyl-1-(phenylamino)propan-2-ol in a similar strategy as that applied for compound 43 .…”

Section: Chemistrymentioning

confidence: 99%

2-(2-Oxo-morpholin-3-yl)-acetamide Derivatives as Broad-Spectrum Antifungal Agents

et al. 2015

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From a fungicidal screen, we identified 2-(2-oxo-morpholin-3-yl)-acetamide derivatives as fungicidal agents against Candida species, additionally characterized by antifungal activity against Aspergillus species. However, development of this series was hampered by low plasmatic stability. Introduction of a gem-dimethyl on the 6-position of the morpholin-2-one core led to considerable improvement in plasmatic stability while maintaining in vitro antifungal activity. Further optimization of the series resulted in the discovery of N-(biphenyl-3-ylmethyl)-2-(4-ethyl-6,6-dimethyl-2-oxomorpholin-3-yl)acetamide (87), which, in addition to fungicidal activity against Candida species, shows promising and broad antifungal in vitro activity against various fungi species, such as molds and dermatophytes. In vivo efficacy was also demonstrated in a murine model of systemic Candida albicans infection with a significant fungal load reduction in kidneys.

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Section: Chemistrymentioning

confidence: 99%