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1. Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia††Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1).

Author

Patrick R. Verhoest, Douglas S. Chapin, Michael Corman, Kari Fonseca, John F. Harms, Xinjun Hou, Eric S. Marr, Frank S. Menniti, Frederick Nelson, Rebecca O’Connor, Jayvardhan Pandit, Caroline Proulx-LaFrance, Anne W. Schmidt, Christopher J. Schmidt, Judith A. Suiciak, and Spiros Liras

Subjects
*PHOSPHODIESTERASE inhibitors, *QUINOLINE, *SCHIZOPHRENIA treatment, *DRUG design, *PYRAZOLES, *DRUG development, *THERAPEUTICS
Abstract

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique “selectivity pocket” for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920). This PDE10A inhibitor is the first reported clinical entry for this mechanism in the treatment of schizophrenia. [ABSTRACT FROM AUTHOR]

Published
2009
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