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Peer-reviewed veterinary case report

Discovery of a novel class of zwitterionic, potent, selective and orally active S1P₁ direct agonists.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2012
Authors:
Aguilar, Nuria et al.
Affiliation:
Almirall Research Center · Spain
Species:
rodent

Abstract

Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural-activity relationships were developed to yield compounds with good selectivity and excellent in vivo efficacy in rat models.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/23141913/