Journal of Medicinal Chemistry · 1996 · 120 citations · 14 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryLead OptimizationStructure-activity RelationshipsHit-to-lead OptimizationLead Compound DesignLead DiscoveryPotency OptimizationReceptor PharmacologySelectivity OptimizationChemical Synthesis Of AnaloguesEndothelin Receptor AntagonistsHigh-throughput Screening AssaysLigand Design For ReceptorsReceptor Binding OptimizationStructure-based Lead DiscoveryStructure-based Ligand DesignStructure-guided Lead Discovery
A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.
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