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Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Oct 01; Vol. 21 (19), pp. 6013-8. Date of Electronic Publication: 2011 Jun 06. - Publication Year :
- 2011
-
Abstract
- S1P(1) receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P(1) receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P(1) receptor agonists.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Butyrates pharmacokinetics
Disease Models, Animal
Dogs
Dose-Response Relationship, Drug
Drug Discovery
Drug Evaluation, Preclinical
Haplorhini
High-Throughput Screening Assays
Humans
Immunosuppressive Agents pharmacokinetics
Indoles pharmacokinetics
Male
Mice
Mice, Inbred BALB C
Nerve Tissue Proteins chemistry
Oxadiazoles pharmacokinetics
RNA-Binding Proteins chemistry
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Substrate Specificity
Autoimmune Diseases drug therapy
Butyrates chemical synthesis
Butyrates pharmacology
Immunosuppressive Agents chemical synthesis
Immunosuppressive Agents pharmacology
Indoles chemical synthesis
Indoles pharmacology
Lymphocytes metabolism
Nerve Tissue Proteins agonists
Oxadiazoles chemical synthesis
Oxadiazoles pharmacology
RNA-Binding Proteins agonists
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21852130
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.05.110