Authors
Deepshikha Patle, Rakesh Chandra Kalita, Motamarri Venkata Naga Lalitha Chaitanya
Published in
Current topics in medicinal chemistry. Mar 13, 2026. Epub Mar 13, 2026.
Abstract
Benzoxazolinone (BOA) and its methoxy analogue, 6-MBOA (Coixol), are privileged heterocyclic scaffolds with diverse pharmacological potential, including neuroprotective, antidiabetic, anti-inflammatory, antimicrobial, and anticancer effects. BOA is a well-studied natural phytoconstituent with broad biological activity, whereas 6-MBOA has received comparatively less attention, despite its emerging biological relevance. The methoxy substitution at the 6-position of 6- MBOA modifies the electronic configuration, enhances lipophilicity, and improves metabolic stability, resulting in superior biological efficacy relative to its parent compound. Among the reported analogues, a benzoxazolinone-based autotaxin inhibitor (compound 26) demonstrated notable potency (IC₅₀;0.019 μM), and several triazole-linked or halogenated derivatives exhibited submicromolar anti-inflammatory and anticancer activities. This review consolidates current knowledge on BOA and 6-MBOA derivatives, focusing on structure-activity relationships, mechanistic underpinnings of bioactivity, and representative synthetic methodologies. Particular attention is given to patented compounds, emphasizing their therapeutic potential and structural innovation. Collectively, these insights establish BOA as a validated pharmacophoric scaffold and highlight 6-MBOA as a promising molecular framework for next-generation drug design and discovery.
PMID:
41832728
Bibliographic data and abstract were imported from PubMed on 15 Mar 2026.
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