Hit-to-lead evaluation of a novel class of sphingosine 1-phosphate lyase inhibitors.
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Summary
A hit-to-lead evaluation of the isoxazolecarboxamide 6, a high-throughput screening hit, as a novel S1P lyase inhibitor is described and it is identified that future lead-optimization efforts to overcome this problem should focus on blocking the N-dealkylation on the secondary amine.
- Type
- article
- Published
- 2016-05-01
- Cited by
- 13
- References
- 26
- Access
- Open access
- OpenAlex
- https://openalex.org/W27020302
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:19555891
Keywords
Computer science
References
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Cited by
- Bacterial versus human sphingosine-1-phosphate lyase (S1PL) in the design of potential S1PL inhibitors.
- Therapeutic Strategies and Pharmacological Tools Influencing S1P Signaling and Metabolism
- Studies on the inhibition of sphingosine-1-phosphate lyase by stabilized reaction intermediates and stereodefined azido phosphates.
- Sphingosine-1-Phosphate (S1P) Lyase Inhibition Causes Increased Cardiac S1P Levels and Bradycardia in Rats
- Characterization of homologous sphingosine-1-phosphate lyase isoforms in the bacterial pathogen Burkholderia pseudomallei
- Synthesis of 2-Vinyl sphingolipids as S1PL inhibitors
- FTY720 Inhibits the Development of Collagen-Induced Arthritis in Mice by Suppressing the Recruitment of CD4+ T Lymphocytes
- Synthesis, characterization, COX1/2 inhibition and molecular modeling studies on novel 2-thio-diarylimidazoles
- Hit-to-lead optimization of 2-aminoquinazolines as anti-microbial agents against Leishmania donovani.
- Inhibiting sphingosine 1-phosphate lyase: From efficacy to mechanism.
- Characterisation of homologous sphingosine 1-phosphate lyase ( S 1 PL ) isoforms in the bacterial pathogen Burkholderia pseudomallei
- DDDT_A_293876 1981..1992
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