Discovery of cariprazine (RGH-188): A novel antipsychotic acting on dopamine D3/D2 receptors

Éva Ágai-Csongor, György Domány, Katalin Nógrádi, +17

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryDopamine D3/d2 ReceptorsPsychoactive DrugPsychiatryFunctional Selectivity +6

Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications

János Galambos, Attila Bielik, Mikhail Krasavin, +20

Journal of Medicinal Chemistry

Psychiatric IndicationsHigh ThroughputPsychopharmacologyPharmacotherapySocial Sciences +18

Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile

Éva Ágai-Csongor, Katalin Nógrádi, János Galambos, +12

Bioorganic & Medicinal Chemistry Letters

PsychiatryMedicineEps ProfilePsychopharmacologySchizophrenia +9

Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists

János Galambos, Gábor Wágner, Katalin Nógrádi, +17

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyBiochemistryFunctional SelectivityMedicineMechanism Of Action +4

4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate

János Galambos, György Domány, Katalin Nógrádi, +13

Bioorganic & Medicinal Chemistry Letters

Negative Allosteric ModulatorsSignal TransductionG Protein-coupled ReceptorMetabotropic Glur5 ReceptorsDevelopment Candidate +7

Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs

Gábor Wágner, Csaba Wéber, O. Nyéki, +14

Bioorganic & Medicinal Chemistry Letters

Chemical EngineeringEngineeringMedicineOrganic ChemistryChemistry +3

Stepwise aromatic nucleophilic substitution in continuous flow. Synthesis of an unsymmetrically substituted 3,5-diamino-benzonitrile library

László Lengyel, Viktor Gyóllai, Tamás Nagy, +7

Molecular Diversity

Engineering3,5-Diamino-benzonitrile LibraryOrganic ChemistryFlow SynthesisChemistry +3

Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization

Katalin Nógrádi, Gábor Wágner, György Domány, +13

Bioorganic & Medicinal Chemistry Letters

Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Hit-to-lead optimization

Katalin Nógrádi, Gábor Wágner, György Domány, +13

Bioorganic & Medicinal Chemistry Letters

Negative Allosteric ModulatorsBiochemistryFunctional SelectivityMetabotropic Glur5 ReceptorsMedicine +8