Results 231 to 240 of about 4,657 (257)

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

Journal of Medicinal Chemistry, 2006
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 ...
Christopher J. Schmidt, Robert D. Williams, John M. Humphrey, Frank S. Menniti, Kimberly G. Estep, Jayvardhan Pandit, Feng V. Yang, Thomas Allen Chappie, Carol B. Fox, Spiros Liras, Lorraine A. Lebel, Meihua Tu, Martin Patrick Allen, Eric S. Marr   +13 more
openaire   +3 more sources

MK-8189: A Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia

Synfacts, 2023

semanticscholar   +1 more source

Expanding the genotype-phenotype landscape of PDE10A-associated movement disorders (S42.004)

Wednesday, April 26, 2023
Saeed Bohlega, Zainah Al-Qahtani, Francisco J. Guzmán-Vega, R. Ramakrishnan, Ali H. Abusrair, Haya Aldosari, A. Aldakheel, Salma Al-Qahtani, D. Monies, Stefan T. Arold   +9 more
semanticscholar   +1 more source

Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies

Bioorganic & Medicinal Chemistry Letters, 2019
A novel series of benzothiophene derivatives was discovered as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity relationship studies on high-throughput screening hit compound 1 led to the identification of 7-acetyl-3-methyl-N-(quinolin-2-yl)-1-benzothiophene-2-carboxamide (16), with potent inhibitory activity (PDE10A IC50 = 7.6 nM) and ...
Minako Tomino, Yasuhiro Hayashi, Yoshiaki Oyama, Kenichi Hiramatsu, Yoshito Kawamoto   +4 more
openaire   +3 more sources

The Use of PDE10A and PDE9 Inhibitors for Treating Schizophrenia

2014
Schizophrenia (Scz) is a chronic and debilitating neurological disorder that afflicts approximately 1% of the general population with an increased incidence within families. Signs of this disorder typically appear between the ages of 16–30 although rare cases of childhood (
Jamison B. Tuttle, Bethany L. Kormos
openaire   +2 more sources

An insight into reactivity and bioactivity properties of quorum sensing peptides against PDE10A: a computational peptidology approach

Journal of Molecular Modeling, 2022
Bhargav Shreevatsa, Chandan Dharmashekara, A. Jain, R. Amachawadi, R. Achar, A. Syed, C. Shivamallu, S. Kollur, J. Frau, N. Flores-Holguín, D. Glossman‐Mitnik   +10 more
semanticscholar   +1 more source

PDE10A knockout mice: Behavioral characterization and effects of papaverine, a PDE10A inhibitor

Schizophrenia Research, 2003
J. Stock, Frank S. Menniti, Sheryl A. McCarthy, Judith A. Siuciak, John F. Harms, A. Shrikhande, C. Strick, J. McNeish, Douglas S. Chapin, L. James, R. D. Williams, S. Wong, Christopher J. Schmidt   +12 more
openaire   +2 more sources

Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.

European journal of medicinal chemistry, 2022
A. Zagórska, Adam Bucki, A. Partyka, M. Jastrzębska-Więsek, A. Siwek, M. Głuch-Lutwin, Barbara Mordyl, Anna Jaromin, M. Walczak, A. Wesołowska, M. Kołaczkowski   +10 more
semanticscholar   +1 more source

Targeting PDE10A in schizophrenia

Drugs of the Future, 2012
B. Langen, N. Hoefgen, C. Grunwald
openaire   +2 more sources

Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition

Journal of Medicinal Chemistry, 2012
Xinjun Hou, Christopher John Helal, Thomas Allen Chappie   +2 more
openaire   +3 more sources