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

Yang SW, Smotryski J, McElroy WT, Tan Z, Ho G, Tulshian D, Greenlee WJ, Guzzi M, Zhang X, Mullins D, Xiao L, Hruza A, Chan TM, Rindgen D, Bleickardt C, Hodgson R
Bioorg Med Chem Lett 22 235-9 (2012)
Cited: 22 times
EuropePMC logo PMID: 22142545

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.

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Reviews citing this publication (8)

  1. Clinical and molecular genetics of the phosphodiesterases (PDEs). Azevedo MF, Faucz FR, Bimpaki E, Horvath A, Levy I, de Alexandre RB, Ahmad F, Manganiello V, Stratakis CA. Endocr Rev 35 195-233 (2014)
  2. Quinoline- and isoquinoline-sulfonamide analogs of aripiprazole: novel antipsychotic agents? Zajdel P, Partyka A, Marciniec K, Bojarski AJ, Pawlowski M, Wesolowska A. Future Med Chem 6 57-75 (2014)
  3. Future directions in phosphodiesterase drug discovery. DeNinno MP. Bioorg Med Chem Lett 22 6794-6800 (2012)
  4. Temporal and spatial regulation of cAMP signaling in disease: role of cyclic nucleotide phosphodiesterases. Otero C, Peñaloza JP, Rodas PI, Fernández-Ramires R, Velasquez L, Jung JE. Fundam Clin Pharmacol 28 593-607 (2014)
  5. 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)
  6. Newer antipsychotics and upcoming molecules for schizophrenia. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA. Eur J Clin Pharmacol 69 1497-1509 (2013)
  7. Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update. Kehler J. Expert Opin Ther Pat 23 31-45 (2013)
  8. 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 (12)

  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. PDE5 Inhibitors as Potential Tools in the Treatment of Cystic Fibrosis. Noel S, Dhooghe B, Leal T. Front Pharmacol 3 167 (2012)
  4. 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)
  5. HPRT-deficiency dysregulates cAMP-PKA signaling and phosphodiesterase 10A expression: mechanistic insight and potential target for Lesch-Nyhan Disease? Guibinga GH, Murray F, Barron N. PLoS One 8 e63333 (2013)
  6. 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)
  7. 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)
  8. 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)
  9. 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)
  10. Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I. Das S, Harde RL, Shelke DE, Khairatkar-Joshi N, Bajpai M, Sapalya RS, Surve HV, Gudi GS, Pattem R, Behera DB, Jadhav SB, Thomas A. Bioorg Med Chem Lett 24 2073-2078 (2014)
  11. 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)
  12. Design and optimization of purine derivatives as in vivo active PDE10A inhibitors. Chen L, Chen D, Tang L, Ren J, Chen J, Zhen X, Liu YC, Zhang C, Luo H, Shen J, Xiong B. Bioorg Med Chem 25 3315-3329 (2017)


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