Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors-Reference-Cited by-同舟云学术

Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors

Published:2012-10-12 Issue:21 Volume:55 Page:9055-9068
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Claffey Michelle M.¹,Helal Christopher J.¹,Verhoest Patrick R.¹,Kang Zhijun¹,Fors Kristina S.¹,Jung Stanley¹,Zhong Jiaying¹,Bundesmann Mark W.¹,Hou Xinjun¹,Lui Shenping¹,Kleiman Robin J.¹,Vanase-Frawley Michelle¹,Schmidt Anne W.¹,Menniti Frank¹,Schmidt Christopher J.¹,Hoffman William E.¹,Hajos Mihaly¹,McDowell Laura¹,O’Connor Rebecca E.¹,MacDougall-Murphy Mary¹,Fonseca Kari R.¹,Becker Stacey L.¹,Nelson Frederick R.¹,Liras Spiros¹

Affiliation:

1. Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm3009635

Reference32 articles.

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).

2. Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors

3. Expression of cGMP-Specific Phosphodiesterase 9A mRNA in the Rat Brain