Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease

Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease

The discovery of a dual MAO-B/SSAO inhibitor PXS-5131 is reported. The compound offers a compact and rigid three-dimensional structure with superior selectivity over MAO-A. Potency and selectivity are linked to both the double bond geometry and stereochemistry of the allylamine moiety, highlighting...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2022-10, Vol.74, p.128942-128942, Article 128942
Hauptverfasser: Foot, Jonathan S., Buson, Alberto, Deodhar, Mandar, Findlay, Alison D., Robertson, Alan D., Turner, Craig I., Yow, Tin, Zhou, Wenbin, Jarolimek, Wolfgang
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Sprache:eng
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Amine oxidase
MAO-A
MAO-B
SSAO
VAP-1
Vinyl fluoride
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container_issue
container_start_page 128942
container_title Bioorganic & medicinal chemistry letters
container_volume 74
creator Foot, Jonathan S.
Buson, Alberto
Deodhar, Mandar
Findlay, Alison D.
Robertson, Alan D.
Turner, Craig I.
Yow, Tin
Zhou, Wenbin
Jarolimek, Wolfgang
description The discovery of a dual MAO-B/SSAO inhibitor PXS-5131 is reported. The compound offers a compact and rigid three-dimensional structure with superior selectivity over MAO-A. Potency and selectivity are linked to both the double bond geometry and stereochemistry of the allylamine moiety, highlighting the importance of optimal set up of these features in the class of amine oxidase inhibitors. PXS-5131 possesses an attractive preclinical pharmacokinetic profile and has anti-inflammatory properties in models of acute inflammation and neuroinflammation. [Display omitted] The discovery of a dual MAO-B/SSAO inhibitor PXS-5131 is reported. The compound offers a compact and rigid three-dimensional structure with superior selectivity over MAO-A. Potency and selectivity are linked to both the double bond geometry and stereochemistry of the allylamine moiety, highlighting the importance of optimal set up of these features in the class of amine oxidase inhibitors. PXS-5131 possesses an attractive preclinical pharmacokinetic profile and has anti-inflammatory properties in models of acute inflammation and neuroinflammation.
doi_str_mv 10.1016/j.bmcl.2022.128942
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1464-3405
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source Elsevier ScienceDirect Journals
subjects Amine oxidase
MAO-A
MAO-B
SSAO
VAP-1
Vinyl fluoride
title Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease
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