Lead Optimization of Thiazolo[5,4-c]piperidines: 3-Cyclobutoxy Linker as a Key Spacer for H3R Inverse Agonists-Reference-Cited by-同舟云学术

Lead Optimization of Thiazolo[5,4-c]piperidines: 3-Cyclobutoxy Linker as a Key Spacer for H3R Inverse Agonists

Published:2012-10-05 Issue:12 Volume:7 Page:2087-2092
ISSN:1860-7179
Container-title:ChemMedChem
language:en
Short-container-title:ChemMedChem

Author:

Provins Laurent,Denonne Frédéric,Célanire Sylvain,Christophe Bernard,Defays Sabine,Delaunoy Christel,Delporte Marie-Laure,Demaude Thierry,Durieu Véronique,Gillard Michel,Hubert Delphine,Lamberty Yves,Lorent Geneviève,Valade Anne,Vanbellinghen Alain,Van houtvin Nathalie

Publisher

Wiley

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology

Reference17 articles.

1. Drug Discovery

2. The histamine H3 receptor: from discovery to clinical trials with pitolisant

3. Discovery of Two Clinical Histamine H3 Receptor Antagonists: trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764)

4. Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3Receptor (H3R) Inverse Agonists

5. Phenyl-oxazoles, a New Family of Inverse Agonists at the H3Histamine Receptor

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1. Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors;Bioorganic & Medicinal Chemistry;2018-12

2. Lead Generation Paved the Way for the Discovery of a Novel H 3 Inverse Agonist Clinical Candidate;Methods and Principles in Medicinal Chemistry;2016-03-04

3. Removal of Human Ether-à-go-go Related Gene (hERG) K+ Channel Affinity through Rigidity: A Case of Clofilium Analogues;Journal of Medicinal Chemistry;2013-11-25