2-Phenylbenzothiazoles featuring heteroaryl sulfonamide end-capping substructures as developable mPGES-1 inhibitors
Creators
- 1. Gazi Univ, Fac Pharm, Dept Pharmaceut Chem, Tac Sok 3, TR-06560 Ankara, Turkiye
- 2. Friedrich Schiller Univ Jena, Inst Pharm, Dept Pharmaceut Med Chem, Jena, Germany
Description
The inhibition of human microsomal prostaglandin E2 (PGE2) synthase-1 (mPGES-1) is a promising therapeutic modality for developing next-generation anti-inflammatory medications. In this study, we present novel 2-phenylbenzothiazole derivatives featuring heteroaryl sulfonamide end-capping substructures as inhibitors of human mPGES-1, with IC50 values in the range of 0.72-3.40 mu M in a cell-free assay of PGE2 formation. Notably, compound 21, featuring a quinoxalinedione ring in its sulfonamide segment, effectively suppresses PGE2 biosynthesis at a low micromolar concentration (IC50 = 0.72 mu M) with exceptional selectivity against cyclooxygenase (COX)-1, COX-2, 5-lipoxygenase (5-LOX), and FLAP. This compound offers a novel chemical scaffold for developing safer and more effective anti-inflammatory agents.
Files
bib-32867909-c6d9-439b-9f67-d7c26dada8da.txt
Files
(257 Bytes)
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