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Literature DB >> 16870427

Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.

Namal C Warshakoon¹, Justin Sheville, Ritu Tiku Bhatt, Wei Ji, Jose L Mendez-Andino, Kenneth M Meyers, Nick Kim, John A Wos, Chrissy Mitchell, Jennifer L Paris, Beth B Pinney, Ofer Reizes, X Eric Hu.

Abstract

A novel series of substituted quinoline analogs were designed and synthesized as potent and selective melanin concentrating hormone (MCH) antagonists. These analogs show potent (nM) activity (12a-k) with a moderate selectivity. Conversely, the conformationally constrained thienopyrimidinone analogs (18a-g) showed improved activity in MCH-1R and selectivity over 5HT2C.

Entities: Chemical Disease Gene

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Year: 2006 PMID： 16870427 DOI： 10.1016/j.bmcl.2006.07.006

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

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Cited

9 in total

1. The neurotherapeutic role of a selenium-functionalized quinoline in hypothalamic obese rats.

Authors: Ethel Antunes Wilhelm; Cristiane Luchese; Karline C Rodrigues; Cristiani F Bortolatto; Ketlyn P da Motta; Renata L de Oliveira; Jaini J Paltian; Roberta Krüger; Silvane S Roman; Silvana P Boeira; Diego Alves
Journal: Psychopharmacology (Berl) Date: 2021-03-19 Impact factor: 4.530

Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.

1. The neurotherapeutic role of a selenium-functionalized quinoline in hypothalamic obese rats.

2. Ligand-free iron-catalyzed benzylic C (sp³)-H amination of methylarenes with N-fluorobenzenesulfonimide.

3. 4-[(2-Chloro-ethyl)amino]quinolinium chloride monohydrate.

4. 7-Chloro-4-[(E)-2-(4-methoxy-benzyl-idene)hydrazin-1-yl]quinoline monohydrate.

5. 7-Chloro-4-[(E)-(3-chloro-benzyl-idene)hydrazinyl]-1λ-quinolinium 3-chloro-benzoate.

6. 7-Chloro-4-[(E)-2-(2-methoxy-benzyl-idene)hydrazin-1-yl]quinoline monohydrate.

7. 7-Chloro-4-[(E)-N'-(4-fluoro-benzyl-idene)hydrazin-yl]quinoline monohydrate.

8. 3-[(E)-(7-Chloro-4-quinol-yl)hydrazono-meth-yl]benzonitrile monohydrate.

9. 7-Chloro-4-(2-hy-droxy-ethyl-amino)-quinolin-1-ium chloride.