Medicinal chemical optimization of fluorescent pyrrole-based COX-2 probes.
Tetrahedron
; 1232022 Sep 24.
Article
em En
| MEDLINE
| ID: mdl-36968982
ABSTRACT
Recent studies have demonstrated the ability of human prostaglandin-endoperoxide synthase 2 (COX-2) to guide the formation of fluorescent pyrroles through the Paal-Knorr reaction resulting in the discovery of a central motif. This initial discovery prompted further exploration of this motif for the design of COX-2 inhibitors through the modifications of the substituents on the pyrrole core. This effort led to the discovery of a set of pyrroles whose activity was comparable to Celecoxib, an orally prescribed nonsteroidal anti-inflammatory COX-2 inhibitor. Furthermore, structure-activity relationship (SAR) data, important for the discovery of COX-2 inhibitors, has been obtained.
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MEDLINE
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En
Ano de publicação:
2022
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Article