ChemMedChem · 2007 · 39 citations · 12 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryLead OptimizationEnzyme InhibitionLigand-based DesignNeurodegenerative Disease PharmacologyNeurodegenerative Disease PharmacotherapyPotency OptimizationStructure-activity Relationship AnalysisDisease-modifying Therapy DevelopmentMechanism-based Drug DesignMedicinal Chemistry Applications
Structure-based drug design was used to incorporate the traditional hydroxyethyl amine aspartyl protease inhibitor motif into 2,3,5-substituted imidazolidin-4-one structures with good BACE-1 enzyme inhibitory potency. These compounds represent a promising drug target for Alzheimer′s disease-modifying therapy and are therefore of interest to the medicinal chemistry community.
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Masayo Yamazaki, William Neway, Tomoyuki Ohe et al. · Journal of Pharmacology and Experimental Therapeutics · 2001 · 237 citations
Medicine, Oncology, Pharmacology +14
Dieter Seebàch, Eusebio Juaristi, David D. Miller et al. · Helvetica Chimica Acta · 1987 · 197 citations