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- Title
Novel 5-Hydroxy, 5-Substituted Benzenesulfonamide Pyrimidine-2,4,6-Triones Attenuate Lipopolysaccharide-Induced Acute Lung Injury via Inhibition of the Gelatinases, MMP-2 and MMP-9.
- Authors
He, Wei; Jiang, Jie; Yu, Ze ‐ Qian; Zhou, Jia ‐ Hua
- Abstract
Preclinical Research A novel series of ten 5 ‐ hydroxy, 5 ‐ substituted benzene sulfonamide pyrimidine ‐ 2,4,6 ‐ triones were synthesized and their structures ascertained using 1H ‐ NMR, 13C ‐ NMR, mass and elemental analysis. These compounds were subsequently tested for inhibition of MMP ‐ 2 and MMP ‐ 9 where most exhibited activity with compound 5i being the most potent against MMP ‐ 2 and MMP ‐ 9 with IC50 values of 2.35 nM and 8.24 nM, respectively. Compound 5i was further analyzed in a mouse LPS ‐ induced acute lung injury model where it had protective activity. Histochemical studies indicated that 5i improved the vascular integrity of the lung. Drug Dev Res 77 : 251 – 257, 2016. © 2016 Wiley Periodicals, Inc.
- Subjects
PYRIMIDINE synthesis; HETEROCYCLIC compounds synthesis; BENZENE compound synthesis; SULFONAMIDES; GELATINASES; LUNG injuries; PHYSIOLOGY
- Publication
Drug Development Research, 2016, Vol 77, Issue 5, p251
- ISSN
0272-4391
- Publication type
Article
- DOI
10.1002/ddr.21319