Literature DB >> 24900180

Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.

James C Barrow1, Kenneth E Rittle1, Thomas S Reger1, Zhi-Qiang Yang1, Phung Bondiskey1, Georgia B McGaughey1, Mark G Bock1, George D Hartman1, Cuyue Tang2, Jeanine Ballard2, Yuhsin Kuo2, Thomayant Prueksaritanont2, Cindy E Nuss3, Scott M Doran3, Steven V Fox3, Susan L Garson3, Richard L Kraus3, Yuxing Li3, Michael J Marino4, Valerie Kuzmick Graufelds4, Victor N Uebele3, John J Renger3.   

Abstract

A novel series of quinazolinone T-type calcium channel antagonists have been prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 by modifications of the 3- and 4-positions of the quinazolinone ring afforded potent and selective antagonists that displayed in vivo central nervous system efficacy in epilepsy and tremor models, as well as significant effects on rat active wake as measured by electrocorticogram.

Entities:  

Keywords:  Quinazolin-2-ones; T-type calcium channel; calcium channel antagonists; electrocorticogram; epilepsy; tremor

Year:  2010        PMID： 24900180      PMCID： PMC4007971          DOI： 10.1021/ml100004r

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  28 in total

1.  Nomenclature of voltage-gated calcium channels.

Authors:  E A Ertel; K P Campbell; M M Harpold; F Hofmann; Y Mori; E Perez-Reyes; A Schwartz; T P Snutch; T Tanabe; L Birnbaumer; R W Tsien; W A Catterall
Journal:  Neuron       Date:  2000-03       Impact factor: 17.173

2.  Neuropsychological deficits in essential tremor: an expression of cerebello-thalamo-cortical pathophysiology?

Authors:  A I Tröster; S P Woods; J A Fields; K E Lyons; R Pahwa; C I Higginson; W C Koller
Journal:  Eur J Neurol       Date:  2002-03       Impact factor: 6.089

3.  State-dependent inhibition of L-type calcium channels: cell-based assay in high-throughput format.

Authors:  Menghang Xia; John P Imredy; Ken S Koblan; Paul Bennett; Thomas M Connolly
Journal:  Anal Biochem       Date:  2004-04-01       Impact factor: 3.365

4.  Bioactivation of 2,3-diaminopyridine-containing bradykinin B1 receptor antagonists: irreversible binding to liver microsomal proteins and formation of glutathione conjugates.

Authors:  Cuyue Tang; Raju Subramanian; Yuhsin Kuo; Sergey Krymgold; Ping Lu; Scott D Kuduk; Christina Ng; Dong-Mei Feng; Chad Elmore; Eric Soli; Jonathan Ho; Mark G Bock; Thomas A Baillie; Thomayant Prueksaritanont
Journal:  Chem Res Toxicol       Date:  2005-06       Impact factor: 3.739

Review 5.  Bursting of thalamic neurons and states of vigilance.

Authors:  Rodolfo R Llinás; Mircea Steriade
Journal:  J Neurophysiol       Date:  2006-03-22       Impact factor: 2.714

Review 6.  Ca(2+) signaling by T-type Ca(2+) channels in neurons.

Authors:  Lucius Cueni; Marco Canepari; John P Adelman; Anita Lüthi
Journal:  Pflugers Arch       Date:  2008-09-11       Impact factor: 3.657

Review 7.  Thalamic T-type Ca2+ channels and NREM sleep.

Authors:  Vincenzo Crunelli; David W Cope; Stuart W Hughes
Journal:  Cell Calcium       Date:  2006-06-13       Impact factor: 6.817

8.  Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Authors:  William D Shipe; James C Barrow; Zhi-Qiang Yang; Craig W Lindsley; F Vivien Yang; Kelly-Ann S Schlegel; Youheng Shu; Kenneth E Rittle; Mark G Bock; George D Hartman; Cuyue Tang; Jeanine E Ballard; Yuhsin Kuo; Emily D Adarayan; Thomayant Prueksaritanont; Matthew M Zrada; Victor N Uebele; Cindy E Nuss; Thomas M Connolly; Scott M Doran; Steven V Fox; Richard L Kraus; Michael J Marino; Valerie Kuzmick Graufelds; Hugo M Vargas; Patricia B Bunting; Martha Hasbun-Manning; Rose M Evans; Kenneth S Koblan; John J Renger
Journal:  J Med Chem       Date:  2008-06-10       Impact factor: 7.446

9.  Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction.

Authors:  G Bertilsson; J Heidrich; K Svensson; M Asman; L Jendeberg; M Sydow-Bäckman; R Ohlsson; H Postlind; P Blomquist; A Berkenstam
Journal:  Proc Natl Acad Sci U S A       Date:  1998-10-13       Impact factor: 11.205

Review 10.  Rodent models of tremor.

Authors:  Hideto Miwa
Journal:  Cerebellum       Date:  2007       Impact factor: 3.648
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  5 in total

1.  Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

Authors:  Zhi-Qiang Yang; Kelly-Ann S Schlegel; Youheng Shu; Thomas S Reger; Rowena Cube; Christa Mattern; Paul J Coleman; Jim Small; George D Hartman; Jeanine Ballard; Cuyue Tang; Yuhsin Kuo; Thomayant Prueksaritanont; Cindy E Nuss; Scott Doran; Steve V Fox; Susan L Garson; Yuxing Li; Richard L Kraus; Victor N Uebele; Adekemi B Taylor; Wei Zeng; Wei Fang; Cynthia Chavez-Eng; Matthew D Troyer; Julie Ann Luk; Tine Laethem; William O Cook; John J Renger; James C Barrow
Journal:  ACS Med Chem Lett       Date:  2010-08-24       Impact factor: 4.345

Review 2.  A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

Authors:  Tao Liu; James P Beck; Junliang Hao
Journal:  RSC Med Chem       Date:  2022-01-19

3.  Photoredox-mediated hydroalkylation and hydroarylation of functionalized olefins for DNA-encoded library synthesis.

Authors:  Shorouk O Badir; Alexander Lipp; Matthias Krumb; María Jesús Cabrera-Afonso; Lisa Marie Kammer; Victoria E Wu; Minxue Huang; Adam Csakai; Lisa A Marcaurelle; Gary A Molander
Journal:  Chem Sci       Date:  2021-08-05       Impact factor: 9.825

4.  Synthesis of substituted 3,4-dihydroquinazolinones via a metal free Leuckart-Wallach type reaction.

Authors:  Suvarna Bokale-Shivale; Mohammad A Amin; Rajiv T Sawant; Marc Y Stevens; Lewend Turanli; Adam Hallberg; Suresh B Waghmode; Luke R Odell
Journal:  RSC Adv       Date:  2020-12-23       Impact factor: 3.361

5.  Microwave Assisted Synthesis of 4-Phenylquinazolin-2(1H)-one Derivatives that Inhibit Vasopressor Tonus in Rat Thoracic Aorta.

Authors:  Rafaela Teixeira; Talita Menengat; Gabriel Andrade; Bruno Cotrim; Cristiano Ponte; Wilson C Santos; Gabriel Resende
Journal:  Molecules       Date:  2020-03-24       Impact factor: 4.411
  5 in total

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