Literature DB >> 22142545

Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.

Shu-Wei Yang1, Jennifer Smotryski, William T McElroy, Zheng Tan, Ginny Ho, Deen Tulshian, William J Greenlee, Mario Guzzi, Xiaoping Zhang, Deborra Mullins, Li Xiao, Alan Hruza, Tze-Ming Chan, Diane Rindgen, Carina Bleickardt, Robert Hodgson.   

Abstract

A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antipsychotic activity in the MK-801 induced hyperactive rat model.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22142545     DOI： 10.1016/j.bmcl.2011.11.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Newer antipsychotics and upcoming molecules for schizophrenia.

Authors:  Melvin George; Radhika Amrutheshwar; Ravi Philip Rajkumar; Shivanand Kattimani; Steven Aibor Dkhar
Journal:  Eur J Clin Pharmacol       Date:  2013-04-02       Impact factor: 2.953

2.  Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.

Authors:  Junfeng Li; Xiang Zhang; Hongjun Jin; Jinda Fan; Hubert Flores; Joel S Perlmutter; Zhude Tu
Journal:  J Med Chem       Date:  2015-10-15       Impact factor: 7.446

Review 3.  Clinical and molecular genetics of the phosphodiesterases (PDEs).

Authors:  Monalisa F Azevedo; Fabio R Faucz; Eirini Bimpaki; Anelia Horvath; Isaac Levy; Rodrigo B de Alexandre; Faiyaz Ahmad; Vincent Manganiello; Constantine A Stratakis
Journal:  Endocr Rev       Date:  2013-12-05       Impact factor: 19.871

Review 4.  1H-Pyrazolo[3,4-b]quinolines: Synthesis and Properties over 100 Years of Research.

Authors:  Andrzej Danel; Ewa Gondek; Mateusz Kucharek; Paweł Szlachcic; Arkadiusz Gut
Journal:  Molecules       Date:  2022-04-26       Impact factor: 4.927

5.  PDE5 Inhibitors as Potential Tools in the Treatment of Cystic Fibrosis.

Authors:  Sabrina Noel; Barbara Dhooghe; Teresinha Leal
Journal:  Front Pharmacol       Date:  2012-09-18       Impact factor: 5.810

6.  HPRT-deficiency dysregulates cAMP-PKA signaling and phosphodiesterase 10A expression: mechanistic insight and potential target for Lesch-Nyhan Disease?

Authors:  Ghiabe-Henri Guibinga; Fiona Murray; Nikki Barron
Journal:  PLoS One       Date:  2013-05-14       Impact factor: 3.240
  6 in total

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