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Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.

Chappie TA, Humphrey JM, Allen MP, Estep KG, Fox CB, Lebel LA, Liras S, Marr ES, Menniti FS, Pandit J, Schmidt CJ, Tu M, Williams RD, Yang FV
J Med Chem 50 182-5 (2007)
Related entries: 2o8h, 2ovv

Cited: 55 times
EuropePMC logo PMID: 17228859

Abstract

A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A.

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  3. Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present). Trabanco AA, Buijnsters P, Rombouts FJ. Expert Opin Ther Pat 26 933-946 (2016)
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  5. Mitochondria in cancer. Grasso D, Zampieri LX, Capelôa T, Van de Velde JA, Sonveaux P. Cell Stress 4 114-146 (2020)
  6. Advances in Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 1: Overview of the Chemical and Biological Research. Jankowska A, Świerczek A, Wyska E, Gawalska A, Bucki A, Pawłowski M, Chłoń-Rzepa G. Curr Drug Targets 20 122-143 (2019)
  7. Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012. Schröder S, Wenzel B, Deuther-Conrad W, Scheunemann M, Brust P. Molecules 21 (2016)
  8. Phosphodiesterase 10A inhibitors: analysis of US/EP patents granted since 2012. Bartolomé-Nebreda JM, Conde-Ceide S, García M. Pharm Pat Anal 4 161-186 (2015)
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  12. PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action? Menniti FS, Chappie TA, Schmidt CJ. Front Neurosci 14 600178 (2020)

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