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Your search keyword '"Jonathan O. Witt"' showing total 3 results
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3 results on '"Jonathan O. Witt"'

1. Discovery, characterization and biological evaluation of a novel ( R )-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D 4 R) antagonists

Author

Corey R. Hopkins, Kayla J. Temple, Andrea L. McCollum, Craig W. Lindsley, Joel M. Harp, Jonathan O. Witt, Miguel A. Hurtado, Daniel E. Jeffries, and Anna L. Blobaum

Subjects
Scaffold, 010405 organic chemistry, Stereochemistry, Chemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, 01 natural sciences, Biochemistry, 0104 chemical sciences, 03 medical and health sciences, 0302 clinical medicine, Dopamine receptor, Drug Discovery, Molecular Medicine, Receptor, Molecular Biology, 030217 neurology & neurosurgery, Biological evaluation
Abstract

Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4 receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.

Published
2016

2. Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists

Author

Corey R. Hopkins, Miguel A. Hurtado, Jonathan O. Witt, Kayla J. Temple, Craig W. Lindsley, Andrea L. McCollum, Daniel E. Jeffries, Eric D. Huseman, Anna L. Blobaum, and Hyekyung C. Plumley

Subjects
medicine.drug_class, Stereochemistry, Morpholines, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, 01 natural sciences, Biochemistry, Article, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Dopamine, Morpholine, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Molecular Biology, 010405 organic chemistry, Receptors, Dopamine D4, Organic Chemistry, Antagonist, Receptor antagonist, Rats, 0104 chemical sciences, chemistry, Dopamine receptor, Microsomes, Liver, Dopamine Antagonists, Molecular Medicine, Selectivity, 030217 neurology & neurosurgery, medicine.drug
Abstract

Herein, we report the synthesis and structure–activity relationship of a series of chiral alkoxymethyl morpholine analogs. Our efforts have culminated in the identification of (S)-2-(((6-chloropyridin-2-yl) oxy)methyl)-4-((6-fluoro-1H-indol-3-yl)methyl)morpholine as a novel potent and selective dopamine D4 receptor antagonist with selectivity against the other dopamine receptors tested (

Published
2016

3. Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D

Author

Daniel E, Jeffries, Jonathan O, Witt, Andrea L, McCollum, Kayla J, Temple, Miguel A, Hurtado, Joel M, Harp, Anna L, Blobaum, Craig W, Lindsley, and Corey R, Hopkins

Subjects
Models, Molecular, Halogenation, Isomerism, Piperidines, Drug Discovery, Receptors, Dopamine D4, Animals, Dopamine Antagonists, Humans, Crystallography, X-Ray, Antipsychotic Agents, Rats
Abstract

Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D

Published
2016

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