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Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2
Bioorg Med Chem. 2021 Mar 24;38:116115. doi: 10.1016/j.bmc.2021.116115. Online ahead of print.ABSTRACTProlyl hydroxylase (PHD) enzymes play a critical role in the cellular responses to hypoxia through their regulation of the hypoxia inducible factor α (HIF-α) transcription factors. PHD inhibitors show promise for the treatment of diseases including anaemia, cardiovascular disease and stroke. In this work, a pharmacophore-based virtual high throughput screen was used to identify novel potential inhibitors of human PHD2. Two moderately potent new inhibitors were discovered, with IC50 values of 4 μM and 23 μM respectively...
Source: Bioorganic and Medicinal Chemistry - April 16, 2021 Category: Chemistry Authors: Nicole L Richardson Laura J O'Malley Daniel Weissberger Anthony Tumber Christopher J Schofield Renate Griffith Nicole M Jones Luke Hunter Source Type: research

α-Aryl-N-aryl nitrones: Synthesis and screening of a new scaffold for cellular protection against an oxidative toxic stimulus.
Abstract Nitrone-containing compounds are commonly employed as spin traps of free radical species in chemical and biological studies. Some molecules as α-phenyl-N-t-butyl nitrone (PBN) and its derivatives have been tested as potential drugs to treat oxidative stress related diseases, as Alzheimer and stroke for example. In this work we report the design and the synthesis of α-aryl-N-aryl nitrones and their cytoprotection profile on human neuroblastoma cells (SH-SY5Y) under induced oxidative stress. All the nine synthesized nitrones showed a significant response at low micromolar concentration. The selected compo...
Source: Bioorganic and Medicinal Chemistry - January 15, 2016 Category: Chemistry Authors: Matias AC, Biazolla G, Cerchiaro G, Keppler AF Tags: Bioorg Med Chem Source Type: research