Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor-Reference-Cited by-同舟云学术

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor

Published:2017-06-16 Issue:13 Volume:60 Page:5673-5698
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Helal Christopher J.¹^ORCID,Arnold Eric P.¹,Boyden Tracey L.¹,Chang Cheng²,Chappie Thomas A.²,Fennell Kimberly F.¹,Forman Michael D.¹,Hajos Mihaly²,Harms John F.²,Hoffman William E.²,Humphrey John M.¹,Kang Zhijun¹,Kleiman Robin J.²,Kormos Bethany L.²,Lee Che-Wah¹,Lu Jiemin¹,Maklad Noha¹,McDowell Laura¹,Mente Scot²,O’Connor Rebecca E.¹,Pandit Jayvardhan¹,Piotrowski Mary¹,Schmidt Anne W.¹,Schmidt Christopher J.²,Ueno Hirokazu¹,Verhoest Patrick R.²,Yang Edward X.¹

Affiliation:

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

2. Pfizer Worldwide Research and Development, 610 Main Street, Cambridge, Massachusetts 02139, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.7b00397

Reference35 articles.

1. Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition

2. 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).