Literature DB >> 22617492

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.

Rong Jiang1, Xinyi Song, Purva Bali, Anthony Smith, Claudia Ruiz Bayona, Li Lin, Michael D Cameron, Patricia H McDonald, Paul J Kenny, Theodore M Kamenecka.   

Abstract

A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22617492      PMCID： PMC3383661          DOI： 10.1016/j.bmcl.2012.04.122

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  19 in total

1.  SB-334867-A: the first selective orexin-1 receptor antagonist.

Authors:  D Smart; C Sabido-David; S J Brough; F Jewitt; A Johns; R A Porter; J C Jerman
Journal:  Br J Pharmacol       Date:  2001-03       Impact factor: 8.739

2.  The orexin system regulates alcohol-seeking in rats.

Authors:  Andrew J Lawrence; Michael S Cowen; Hong-Ju Yang; Feng Chen; Brian Oldfield
Journal:  Br J Pharmacol       Date:  2006-06-05       Impact factor: 8.739

3.  Role for hypocretin in mediating stress-induced reinstatement of cocaine-seeking behavior.

Authors:  Benjamin Boutrel; Paul J Kenny; Sheila E Specio; Rémi Martin-Fardon; Athina Markou; George F Koob; Luis de Lecea
Journal:  Proc Natl Acad Sci U S A       Date:  2005-12-15       Impact factor: 11.205

Review 4.  Eating, sleeping and rewarding: orexin receptors and their antagonists.

Authors:  Matilda J Bingham; Jiaqiang Cai; Maureen R Deehan
Journal:  Curr Opin Drug Discov Devel       Date:  2006-09

5.  Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.

Authors:  T Sakurai; A Amemiya; M Ishii; I Matsuzaki; R M Chemelli; H Tanaka; S C Williams; J A Richarson; G P Kozlowski; S Wilson; J R Arch; R E Buckingham; A C Haynes; S A Carr; R S Annan; D E McNulty; W S Liu; J A Terrett; N A Elshourbagy; D J Bergsma; M Yanagisawa
Journal:  Cell       Date:  1998-03-06       Impact factor: 41.582

6.  The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity.

Authors:  L de Lecea; T S Kilduff; C Peyron; X Gao; P E Foye; P E Danielson; C Fukuhara; E L Battenberg; V T Gautvik; F S Bartlett; W N Frankel; A N van den Pol; F E Bloom; K M Gautvik; J G Sutcliffe
Journal:  Proc Natl Acad Sci U S A       Date:  1998-01-06       Impact factor: 11.205

7.  Direct involvement of orexinergic systems in the activation of the mesolimbic dopamine pathway and related behaviors induced by morphine.

Authors:  Minoru Narita; Yasuyuki Nagumo; Seiko Hashimoto; Michiko Narita; Junaidi Khotib; Mayumi Miyatake; Takeshi Sakurai; Masashi Yanagisawa; Tomoya Nakamachi; Seiji Shioda; Tsutomu Suzuki
Journal:  J Neurosci       Date:  2006-01-11       Impact factor: 6.167

8.  Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.

Authors:  Christopher J Winrow; Anthony L Gotter; Christopher D Cox; Scott M Doran; Pamela L Tannenbaum; Michael J Breslin; Susan L Garson; Steven V Fox; Charles M Harrell; Joanne Stevens; Duane R Reiss; Donghui Cui; Paul J Coleman; John J Renger
Journal:  J Neurogenet       Date:  2011-04-08       Impact factor: 1.250

9.  A role for lateral hypothalamic orexin neurons in reward seeking.

Authors:  Glenda C Harris; Mathieu Wimmer; Gary Aston-Jones
Journal:  Nature       Date:  2005-08-14       Impact factor: 49.962

10.  2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.

Authors:  Jian Jin; Yonghui Wang; Feng Wang; Dongchuan Shi; Karl F Erhard; Zining Wu; Brian F Guida; Sarah K Lawrence; David J Behm; Jyoti Disa; Kalindi S Vaidya; Christopher Evans; Lynette J McMillan; Ralph A Rivero; Michael J Neeb; Stephen A Douglas
Journal:  Bioorg Med Chem Lett       Date:  2008-04-08       Impact factor: 2.823
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  6 in total

1.  Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor.

Authors:  David A Perrey; Nadezhda A German; Ann M Decker; David Thorn; Jun-Xu Li; Brian P Gilmour; Brian F Thomas; Danni L Harris; Scott P Runyon; Yanan Zhang
Journal:  ACS Chem Neurosci       Date:  2015-02-12       Impact factor: 4.418

2.  Synthesis and Evaluation of Orexin-1 Receptor Antagonists with Improved Solubility and CNS Permeability.

Authors:  David A Perrey; Ann M Decker; Yanan Zhang
Journal:  ACS Chem Neurosci       Date:  2017-11-20       Impact factor: 4.418

3.  An efficient synthesis of cis-4-hydroxyphosphonic and cis-4-hydroxyphosphinic analogs of pipecolic acid from cyclic enaminones.

Authors:  Rubén Oswaldo Argüello-Velasco; Juan Carlos Morales-Solís; Misael Muñoz-Vidales; José Luis Viveros-Ceballos; Ivan Romero-Estudillo; Mario Ordóñez
Journal:  Amino Acids       Date:  2022-01-16       Impact factor: 3.520

Review 4.  Therapeutics development for addiction: Orexin-1 receptor antagonists.

Authors:  David A Perrey; Yanan Zhang
Journal:  Brain Res       Date:  2018-08-24       Impact factor: 3.252

5.  Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.

Authors:  David A Perrey; Nadezhda A German; Brian P Gilmour; Jun-Xu Li; Danni L Harris; Brian F Thomas; Yanan Zhang
Journal:  J Med Chem       Date:  2013-08-26       Impact factor: 7.446

Review 6.  Orexin 1 receptor antagonists in compulsive behavior and anxiety: possible therapeutic use.

Authors:  Emilio Merlo Pich; Sergio Melotto
Journal:  Front Neurosci       Date:  2014-02-13       Impact factor: 4.677
  6 in total

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