Synthesis, Biological Properties, and Molecular Modeling Investigations of Novel 3,4-Diarylpyrazolines as Potent and Selective CB₁ Cannabinoid Receptor Antagonists

Jos H.M. Lange, Hein K. A. C. Coolen, Herman H. van Stuivenberg, +15

Journal of Medicinal Chemistry

Drug TargetBiological PropertiesX-ray Diffraction StudyPharmacotherapyMolecular Modeling Investigations +19

Bioisosteric Replacements of the Pyrazole Moiety of Rimonabant:  Synthesis, Biological Properties, and Molecular Modeling Investigations of Thiazoles, Triazoles, and Imidazoles as Potent and Selective CB₁Cannabinoid Receptor Antagonists

Jos H.M. Lange, Herman H. van Stuivenberg, Hein K. A. C. Coolen, +9

Journal of Medicinal Chemistry

Pyrazole SeriesOrganic ChemistryPharmacotherapyMolecular Modeling InvestigationsChemistry +17

Design, Synthesis and Biological Activity of Rigid Cannabinoid CB1 Receptor Antagonists.

Axel R. Stoit, Jos H.M. Lange, Arnold P. den Hartog, +6

Chemical and Pharmaceutical Bulletin

Pyrazole Ring ClosurePharmacotherapyHeterocycle ChemistryCannabinoid PharmacologyPharmaceutical Chemistry +17

Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity

Jos H.M. Lange, Herman H. van Stuivenberg, Willem Veerman, +6

Bioorganic & Medicinal Chemistry Letters

Cannabis UseMolecular PharmacologyMedicinal ChemistryDrug TargetBiochemistry +10

Synthesis, Structure−Activity Relationships, and Biological Properties of 1-Heteroaryl-4-[ω-(1<i>H</i>-indol-3-yl)alkyl]piperazines, Novel Potential Antipsychotics Combining Potent Dopamine D₂ Receptor Antagonism with Potent Serotonin Reuptake Inhibition

Pieter Smid, Hein K. A. C. Coolen, Hiskias G. Keizer, +13

Journal of Medicinal Chemistry

PsychopharmacologyBiological PropertiesPharmacotherapyChemistryHeterocycle Chemistry +16

Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies

Jos H.M. Lange, Martina A.W. van der Neut, Henri C. Wals, +8

Bioorganic & Medicinal Chemistry Letters

Cannabis UseMedicinal ChemistryDrug TargetBiochemistryMedicine +9

Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB1 receptor antagonists

Jos H.M. Lange, Martina A.W. van der Neut, Arnold P. den Hartog, +5

Bioorganic & Medicinal Chemistry Letters

1,3,5-Trisubstituted 4,5-DihydropyrazolesIntramolecular HydrogenMedicinal ChemistryCannabis UseFunctional Selectivity +7

Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern

Jos H.M. Lange, Martina A.W. van der Neut, Alice J. M. Borst, +3

Bioorganic & Medicinal Chemistry Letters

Cannabis UseDrug TargetBiochemistryFunctional SelectivityMedicine +6

SAR Study of 1-Aryl-4-(phenylarylmethyl)piperazines as Ligands for Both Dopamine D2 and Serotonin 5-HT1A Receptors Showing Varying Degrees of (Ant)agonism. Selection of a Potential Atypical Antipsychotic

R. Feenstra, Adri van den Hoogenband, Cornelis Nicolaas Jozef Stroomer, +5

Chemical and Pharmaceutical Bulletin

Drug TargetBoth Dopamine D2PsychopharmacologyDrug Candidate Slv313Receptor Antagonism +14