Abstract
Aim: Inducible nitric oxide synthase (iNOS) is a validatedtargetfor anti-inflammatory treatment. Based on the authors' previous work,novel aza-ursolic acid derivatives were designedand synthesizedandtheir inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) release from RAW264.7 cells wasevaluated. Materials & results: 16 novel derivatives were screened for their in vitro inhibitory activity against NO release using Griess assaysand the cytotoxicity was evaluated using MTT assays. The presence of furoxan joined to theA-ring of ursolic acid and N-methylpiperazine groups in the lead compound was identified for anti-inflammatory activity, and compound21b showed 94.96% inhibition of NO release at 100μM with an IC50 value of 8.58μM. Conclusion: Compound 21b has potential anti-inflammatory activity with low cytotoxicity that warrants further preclinical study and evaluation.
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