Developing Metal-Binding Isosteres of 8-Hydroxyquinoline as Metalloenzyme Inhibitor Scaffolds.
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DOI: 10.1021/acs.inorgchem.2c00891
Abstract: The use of metal-binding pharmacophores (MBPs) in fragment-based drug discovery has proven effective for targeted metalloenzyme drug development. However, MBPs can still suffer from pharmacokinetic liabilities. Bioisostere replacement is an effective strategy utilized by medicinal… read more here.
Keywords: chemistry; metalloenzyme inhibitor; binding isosteres; drug ... See more keywords
Salicylate metal-binding isosteres as fragments for metalloenzyme inhibition
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DOI: 10.1039/d1sc06011b
Abstract: Metalloenzyme inhibitors typically share a common need to possess a metal-binding pharmacophore (MBP) for binding the active site metal ions. However, MBPs can suffer from physicochemical liabilities, impeding the pharmacological properties and drug-likeliness of inhibitors.… read more here.
Keywords: inhibition; salicylate metal; activity; binding isosteres ... See more keywords