50496-54-3Relevant academic research and scientific papers
Discovery of a novel series of N-hydroxypyridone derivatives protecting astrocytes against hydrogen peroxide-induced toxicity via improved mitochondrial functionality
Singh, Sarbjit,Goo, Ja-Il,Noh, Hyojin,Lee, Sung Jae,Kim, Myoung Woo,Park, Hyejun,Jalani, Hitesh B.,Lee, Kyeong,Kim, Chunsook,Kim, Won-Ki,Ju, Chung,Choi, Yongseok
, p. 1394 - 1405 (2017)
Astrocytes play a key role in brain homeostasis, protecting neurons against neurotoxic stimuli such as oxidative stress. Therefore, the neuroprotective therapeutics that enhance astrocytic functionality has been regarded as a promising strategy to reduce brain damage. We previously reported that ciclopirox, a well-known antifungal N-hydroxypyridone compound, protects astrocytes from oxidative stress by enhancing mitochondrial function. Using the N-hydroxypyridone scaffold, we have synthesized a series of cytoprotective derivatives. Mitochondrial activity assay showed that N-hydroxypyridone derivatives with biphenyl group have comparable to better protective effects than ciclopirox in astrocytes exposed to H2O2. N-hydroxypyridone derivatives, especially 11g, inhibited H2O2-induced deterioration of mitochondrial membrane potential and oxygen consumption rate, and significantly improved cell viability of astrocytes. The results indicate that the N-hydroxypyridone motif can provide a novel cytoprotective scaffold for astrocytes via enhancing mitochondrial functionality.
The chemistry of antimicrobially active 1-hydroxy-2-pyridones
Lohaus,Dittmar
, p. 1311 - 1316 (2007/10/02)
The unsaturated δ-keto esters obtained by condensation of acid chlorides with esters of di- or trialkyl-acrylic acids can be cyclized with hydroxylamine to yield 1-hydroxy-2-pyridones. However, in many cases a two-steps synthesis may be of advantage in preparative respect, the ketoesters being cyclized to 2-pyrones, which then are reacted with hydroxylamine in the presence of certain bases to give. The hydroxy-pyridones show pronounced antifungal activity in vitro as well as in experimental guinea pig dermatophytosis.
Process for the preparation of 1-hydroxy-pyridones
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, (2008/06/13)
Method for making 6-substituted-1-hydroxy-2-pyridones, which may also be substituted in one or more of the 3-, 4-, and 5-positions, by reaction of the corresponding 2-pyrone with hydroxylamine or its salts in the presence of imidazole or a 2-aminopyridine which may be mono- or di-methyl substituted.
