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The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.

Ho GD, Yang SW, Smotryski J, Bercovici A, Nechuta T, Smith EM, McElroy W, Tan Z, Tulshian D, McKittrick B, Greenlee WJ, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R
Bioorg Med Chem Lett 22 1019-22 (2012)
Cited: 16 times
EuropePMC logo PMID: 22222034

Abstract

High-throughput screening identified a series of pyrazoloquinolines as PDE10A inhibitors. The SAR development led to the discovery of compound 27 as a potent, selective, and orally active PDE10A inhibitor. Compound 27 inhibits MK-801 induced hyperactivity at 3mg/kg with an ED(50) of 4mg/kg and displays a ∼6-fold separation between the ED(50) for inhibition of MK-801 induced hyperactivity and hypolocomotion in rats.

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Reviews citing this publication (4)

  1. Advances in Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 1: Overview of the Chemical and Biological Research. Jankowska A, Świerczek A, Wyska E, Gawalska A, Bucki A, Pawłowski M, Chłoń-Rzepa G. Curr Drug Targets 20 122-143 (2019)
  2. Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update. Kehler J. Expert Opin Ther Pat 23 31-45 (2013)
  3. 1H-Pyrazolo[3,4-b]pyridines: Synthesis and Biomedical Applications. Donaire-Arias A, Montagut AM, Puig de la Bellacasa R, Estrada-Tejedor R, Teixidó J, Borrell JI. Molecules 27 2237 (2022)
  4. 1H-Pyrazolo[3,4-b]quinolines: Synthesis and Properties over 100 Years of Research. Danel A, Gondek E, Kucharek M, Szlachcic P, Gut A. Molecules 27 2775 (2022)

Articles citing this publication (9)

  1. Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition. Hamaguchi W, Masuda N, Isomura M, Miyamoto S, Kikuchi S, Amano Y, Honbou K, Mihara T, Watanabe T. Bioorg Med Chem 21 7612-7623 (2013)
  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. Li J, Zhang X, Jin H, Fan J, Flores H, Perlmutter JS, Tu Z. J Med Chem 58 8584-8600 (2015)
  3. Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux. Rzasa RM, Hu E, Rumfelt S, Chen N, Andrews KL, Chmait S, Falsey JR, Zhong W, Jones AD, Porter A, Louie SW, Zhao X, Treanor JJ, Allen JR. Bioorg Med Chem Lett 22 7371-7375 (2012)
  4. Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability. Chino A, Masuda N, Amano Y, Honbou K, Mihara T, Yamazaki M, Tomishima M. Bioorg Med Chem 22 3515-3526 (2014)
  5. Synthesis, SAR study, and biological evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors with reduced CYP3A4 inhibition. Hamaguchi W, Masuda N, Miyamoto S, Shiina Y, Kikuchi S, Mihara T, Moriguchi H, Fushiki H, Murakami Y, Amano Y, Honbou K, Hattori K. Bioorg Med Chem 23 297-313 (2015)
  6. Antagonism of the adenosine A2A receptor attenuates akathisia-like behavior induced with MP-10 or aripiprazole in a novel non-human primate model. Bleickardt CJ, Kazdoba TM, Jones NT, Hunter JC, Hodgson RA. Pharmacol Biochem Behav 118 36-45 (2014)
  7. Addressing phototoxicity observed in a novel series of biaryl derivatives: discovery of potent, selective and orally active phosphodiesterase 10A inhibitor ASP9436. Hamaguchi W, Masuda N, Miyamoto S, Kikuchi S, Narazaki F, Shiina Y, Seo R, Amano Y, Mihara T, Moriguchi H, Hattori K. Bioorg Med Chem 23 3351-3367 (2015)
  8. Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors. Banerjee A, Narayana L, Raje FA, Pisal DV, Kadam PA, Gullapalli S, Kumar H, More SV, Bajpai M, Sangana RR, Jadhav S, Gudi GS, Khairatkar-Joshi N, Merugu RR, Voleti SR, Gharat LA. Bioorg Med Chem Lett 23 6747-6754 (2013)
  9. Inhibition mechanism exploration of quinoline derivatives as PDE10A inhibitors by in silico analysis. Wu Q, Gao Q, Guo H, Li D, Wang J, Gao W, Han C, Li Y, Yang L. Mol Biosyst 9 386-397 (2013)


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