Literature DB >> 29870883

Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.

Rafał Moszczyński-Pętkowski1, Jakub Majer2, Małgorzata Borkowska2, Łukasz Bojarski3, Sylwia Janowska3, Mikołaj Matłoka3, Filip Stefaniak2, Damian Smuga2, Katarzyna Bazydło3, Krzysztof Dubiel2, Maciej Wieczorek3.   

Abstract

New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  1H-1,3-benzodiazoles; Imidazo[1,2-a]pyrimidines; PDE10A

Mesh:

Substances:

Year:  2018        PMID: 29870883     DOI: 10.1016/j.ejmech.2018.05.043

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Structure-based discovery and bio-evaluation of a cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-one as a phosphodiesterase 10A inhibitor.

Authors:  Mayasah Al-Nema; Anand Gaurav; Vannajan Sanghiran Lee; Baskaran Gunasekaran; Ming Tatt Lee; Patrick Okechukwu; Piyarat Nimmanpipug
Journal:  RSC Adv       Date:  2022-01-11       Impact factor: 3.361

2.  Quetiapine and novel PDE10A inhibitors potentiate the anti-BuChE activity of donepezil.

Authors:  Joanna Sikora; Maria Podsiedlik; Tadeusz Pietras; Marcin Kosmalski; Mikołaj Matłoka; Rafał Moszczyński-Petkowski; Maciej Wieczorek; Magdalena Markowicz-Piasecka
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

  2 in total

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