Stability-Indicating Assay of Novel 5-(Hydroxamic acid)methyl Oxazolidinones with 5-Lipooxygenase Inhibitory Activity
Hessa M. Al-Mutairi, Oludotun A. Phillips, Naser F. Al-Tannak
TL;DR
Researchers developed a method to test the stability of new oxazolidinone compounds that inhibit a key enzyme in inflammation and allergies.
Contribution
The paper introduces a validated stability-indicating assay for novel oxazolidinone derivatives with 5-lipooxygenase inhibitory activity.
Findings
The compounds were stable in human plasma and thermal conditions with 82–90% extraction recoveries.
They were unstable in acidic, basic, and oxidative conditions.
The compounds show promise for treating inflammatory and allergic diseases.
Abstract
Background: Oxazolidinone derivatives are a novel class of synthetic antibacterial agents, characterized by a five-membered heterocyclic ring containing oxygen and nitrogen and a carbonyl functionality at position 2. This pharmacophore is responsible not only for antibacterial activity but also for a variety of other biological activities, including anticancer activity, anticoagulant activity, and several others. A series of novel oxazolidinone derivatives containing a hydroxamic acid moiety were synthesized in our laboratories and identified as potent inhibitors of the enzyme 5-lipoxygenase (5-LO), a key enzyme involved in the biosynthesis of leukotrienes (LTs). LTs are proinflammatory mediators implicated in allergic and inflammatory diseases. Currently, zileuton is the only FDA-approved 5-LO inhibitor, emphasizing the need to develop new agents for the treatment of such diseases.…
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Taxonomy
TopicsSynthesis and Reactions of Organic Compounds · Macrophage Migration Inhibitory Factor · Inflammatory mediators and NSAID effects