Four series of total 35 new pyrazolo[4,3-]pyrimidine compounds were designed, synthesized and evaluated for their inhibitory activity against LPS-induced NO production in RAW264.7 macrophages. Among them, compound was found to be the most potent inhibitor, which decreased the production of cytokines , such as NO, IL-6 and TNF-α, with IC values of 2.64, 4.38 and 5.63 μM, respectively. Further studies showed that compound inhibited cytokines secretion of macrophages through suppressing TLR4/p38 signaling pathway. Additionally, compound showed anti-inflammatory activity in LPS-induced model of acute lung injury. These data suggested that compound may be a promising lead structure for the treatment of ALI.
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| http://dx.doi.org/10.1080/14756366.2019.1618291 | DOI Listing |
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