Wen Peng, Jianru Liu, Zhen Li, Yuanan Wang, Yangqian Sun, Yanzhao Chen, David J. Lefer, Weiwei Guo, Yueqin Zheng
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引用次数: 0
Abstract
The physiological and pharmacological benefits of hydrogen sulfide (H2S) are well established, and various H2S and persulfide donors have been developed. However, few studies have examined the in vivo pharmacokinetics of sulfur donors, as most activity and metabolism tests are conducted in vitro, limiting insights into their clinical applications. This study utilized butylphthalide (NBP), an approved drug for ischemic stroke, by integrating H2S and persulfide moieties directly into NBP’s carbonyl groups. We systematically compared drug metabolism in vitro and in vivo and evaluated donor efficacy in ischemia-reperfusion models. Results revealed notable in vitro/in vivo metabolic differences, with thioacid-containing donors showing promising therapeutic effects in cerebral ischemia, reducing infarct size, oxidative stress, and neuronal apoptosis.
期刊介绍：
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.
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