Literature DB >> 21087867

Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.

Battistina Asproni1, Gabriele Murineddu, Amedeo Pau, Gérard A Pinna, Morten Langgård, Claus Tornby Christoffersen, Jacob Nielsen, Jan Kehler.   

Abstract

A series of phenylimidazole-pyrazolo[1,5-c]quinazolines 1a-q was designed, synthesized and characterised as a novel class of potent phophodiesterase 10A (PDE10A) inhibitors. In this series, 2,9-dimethyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)ethyl)pyrazolo[1,5-c]quinazoline (1q) showed the highest affinity for PDE10A enzyme (IC(50)=16nM).
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 21087867     DOI: 10.1016/j.bmc.2010.10.038

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.

Authors:  Hao Yang; Francis N Murigi; Zhijian Wang; Junfeng Li; Hongjun Jin; Zhude Tu
Journal:  Bioorg Med Chem Lett       Date:  2014-12-22       Impact factor: 2.823

Review 2.  A comprehensive review in improving delivery of small-molecule chemotherapeutic agents overcoming the blood-brain/brain tumor barriers for glioblastoma treatment.

Authors:  Da Wang; Chao Wang; Liang Wang; Yue Chen
Journal:  Drug Deliv       Date:  2019-12       Impact factor: 6.419

3.  2-(4-Bromo-phen-yl)-N-[3-(1H-imidazol-1-yl)prop-yl]quinazolin-4-amine.

Authors:  Marcia Pérez-Fehrmann; Victor Kesternich; Felipe Verdugo; Philippe Christen; Céline Besnard
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-30

4.  Synthesis and evaluation of imidazole-4,5- and pyrazine-2,3-dicarboxamides targeting dengue and yellow fever virus.

Authors:  Milind Saudi; Joanna Zmurko; Suzanne Kaptein; Jef Rozenski; Johan Neyts; Arthur Van Aerschot
Journal:  Eur J Med Chem       Date:  2014-09-22       Impact factor: 6.514

  4 in total

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