Chuang Xia

Discovery of Novel Natural Product-Based PDE4 Inhibitors for Ischemic Stroke Treatment without Emetogenicity at Ultra-High Doses

Chuang Xia, Mingjia Yu, Yujie Ni, Shanfang Fang et autres

Phosphodiesterase-4 (PDE4) inhibitors show potential for treating ischemic stroke, but are often constrained by emesis or low blood-brain barrier (BBB) permeability. To overcome these challenges, this paper developed novel PDE4 inhibitors via AI-driven structural evolution of natural antistroke products and identified the …

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Discovery of novel pyrrolopyrimidine-based PDE7 inhibitors against alcoholic liver injury

Jiaxi Huang, Chuang Xia, L. Li, Huichang Bi et autres

A novel PDE4 inhibitor ZX21011 alleviates neuronal apoptosis by decreasing GSK3β-mediated Drp1 Ser616 phosphorylation in cerebral ischemia reperfusion

Huizhen Wen, Xingxing Tu, Fulan Luo, Chunyuan Zeng et autres

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Discovery of novel N2-indazole derivatives as phosphodiesterase 4 inhibitors for the treatment of inflammatory bowel disease

Lei Zheng, Kun Chen, Yifan Xie, Jiaxi Huang et autres

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Discovery of 7-alkoxybenzofurans as PDE4 inhibitors with hepatoprotective activity in D-GalN/LPS-induced hepatic sepsis

Chuang Xia, Huizhen Wen, Lei Zheng, Yujie Ni et autres

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Discovery of 7-Alkoxybenzofurans as Pde4 Inhibitors with Hepatoprotective Activity in D-Galn/Lps-Induced Hepatic Sepsis

Chuang Xia, Huizhen Wen, Lei Zheng, Yujie Ni et autres

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Discovery of 4-Ethoxy-6-chloro-5-azaindazoles as Novel PDE4 Inhibitors for the Treatment of Alcohol Use Disorder and Alcoholic Liver Diseases

Lei Zheng, Zulihuma Aimaiti, Lu Long, Chuang Xia et autres

Alcohol use disorder (AUD) results in numerous disabilities and approximately 3 million deaths annually, caused mainly by alcoholic liver disease (ALD). Phosphodiesterase IV (PDE4) has emerged as an attractive molecular target for a new treatment for AUD and ALD. In this study, …

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Discovery of Novel 3-Amino-4-alkoxyphenylketones as PDE4 Inhibitors with Improved Oral Bioavailability and Safety against Spatial Memory Impairments

Chuang Xia, Jiapeng He, Kai-Wen Feng, Lu Liu et autres

To realize PDE4 inhibitors with good developmental potentiality for the treatment of dementia, structure-based optimizations of lead compound FCPR03 resulted in novel aminophenylketones 9c and 9H with low nanomolar potency, which displayed comparable activity to rolipram, satisfactory bioavailability ( F % = …

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