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Literature DB >> 22607676

Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists.

Gopi Kumar Mittapalli¹, Danielle Vellucci, Jun Yang, Marion Toussaint, Shaun P Brothers, Claes Wahlestedt, Edward Roberts.

Abstract

Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC(50) values of 19 nM and 12 nM respectively.

Entities: Chemical Disease Gene Species

Mesh：

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Year: 2012 PMID： 22607676 PMCID： PMC3362798 DOI： 10.1016/j.bmcl.2012.04.107

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

18 in total

Review 1. Emerging functions of neuropeptide Y Y(2) receptors in the brain.

Authors: T Kaga; M Fujimiya; A Inui
Journal: Peptides Date: 2001-03 Impact factor: 3.750

2. Novel non-peptidic neuropeptide Y Y2 receptor antagonists.

Authors: Jill A Jablonowski; Wenying Chai; Xiaobing Li; Dale A Rudolph; William V Murray; Mark A Youngman; Scott L Dax; Diane Nepomuceno; Pascal Bonaventure; Timothy W Lovenberg; Nicholas I Carruthers
Journal: Bioorg Med Chem Lett Date: 2004-03-08 Impact factor: 2.823

3. The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.

Authors: Gillian E Lunniss; Ashley A Barnes; Nick Barton; Matteo Biagetti; Federica Bianchi; Stephen M Blowers; Laura L Caberlotto; Amanda Emmons; Ian P Holmes; Dino Montanari; Roz Norris; Gemma V Puckey; Dewi J Walters; Steve P Watson; John Willis
Journal: Bioorg Med Chem Lett Date: 2010-11-10 Impact factor: 2.823

4. The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.

Authors: Gillian E Lunniss; Ashley A Barnes; Nick Barton; Matteo Biagetti; Federica Bianchi; Stephen M Blowers; Laura Caberlotto; Amanda Emmons; Ian P Holmes; Dino Montanari; Ros Norris; Dewi J Walters; Steve P Watson
Journal: Bioorg Med Chem Lett Date: 2009-06-13 Impact factor: 2.823

5. Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.

Authors: Shaun P Brothers; S Adrian Saldanha; Timothy P Spicer; Michael Cameron; Becky A Mercer; Peter Chase; Patricia McDonald; Claes Wahlestedt; Peter S Hodder
Journal: Mol Pharmacol Date: 2009-10-16 Impact factor: 4.436

6. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.

Authors: Devin M Swanson; Victoria D Wong; Jill A Jablonowski; Chandra Shah; Dale A Rudolph; Curt A Dvorak; Mark Seierstad; Lisa K Dvorak; Kirsten Morton; Diane Nepomuceno; John R Atack; Pascal Bonaventure; Timothy W Lovenberg; Nicholas I Carruthers
Journal: Bioorg Med Chem Lett Date: 2011-07-18 Impact factor: 2.823

Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists.

Review 1. Emerging functions of neuropeptide Y Y(2) receptors in the brain.

2. Novel non-peptidic neuropeptide Y Y2 receptor antagonists.

3. The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.

4. The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.

5. Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.

6. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.

7. Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze.

8. Neuropeptide Y receptor antagonists.

Review 9. G protein-coupled receptors in major psychiatric disorders.

10. Differentially functionalized diamines as novel ligands for the NPY2 receptor.

Review 1. PET Imaging of the Neuropeptide Y System: A Systematic Review.

Review 2. Ligands of the neuropeptide Y Y2 receptor.

3. Neuropeptide Y receptors: how to get subtype selectivity.