873051-19-5Relevant articles and documents
Synthesis and biological evaluation of 4-oxoquinoline-3-carboxamides derivatives as potent anti-fibrosis agents
Zhu, Jun,He, Lin,Ma, Liang,Wei, Zhe,He, Jiqiang,Yang, Zhuang,Pu, Yuzhi,Cao, Dong,Wu, Yuzhe,Xiang, Mingli,Peng, Aihua,Wei, Yuquan,Chen, Lijuan
, p. 5666 - 5670 (2015/01/08)
Thirty-one 4-oxoquinoline-3-carboxamides derivatives were synthesized and evaluated for their anti-fibrotic activities by the inhibition of TGF-β1-induced total collagen accumulation and anti-inflammatory activities by the inhibition of LPS-stimulated TNF-α production. Among them, three compounds (10a, 10l and 11g) exhibited potent inhibitory effects on both TGF-β1-induced total collagen accumulation and LPS-stimulated TNF-α production. Furthermore, oral administrations of 10l at a dose of 20 mg/kg/day for 4 weeks effectively alleviated lung inflammation and injury, and decreased lung collagen accumulation in bleomycin-induced pulmonary fibrosis model. Histopathological evaluation of lung tissue confirmed 10l as a potential, orally active agent for the treatment of pulmonary fibrosis.
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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Page/Page column 232, (2008/06/13)
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.