Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats-Reference-Cited by-同舟云学术

Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats

Published:2024 Issue:1 Volume:15 Page:344-354
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Brotschi Christine¹^ORCID,Bolli Martin H.¹^ORCID,Gatfield John¹^ORCID,Roch Catherine¹^ORCID,Sifferlen Thierry¹^ORCID,Treiber Alexander¹^ORCID,Williams Jodi T.¹^ORCID,Boss Christoph¹^ORCID

Affiliation:

1. Idorsia Pharmaceuticals Ltd, Drug Discovery and Preclinical Development, Hegenheimermattweg 91, 4123 Allschwil, Basel-Landschaft, Switzerland

Abstract

Medicinal chemistry efforts starting from the GPCR agonist HTS hit 1 led to the discovery of the potent, selective, brain-penetrating, orally active orexin 2 receptor antagonists 43 that induced sleep in rats.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2024/MD/D3MD00573A

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