1. Synthesis and evaluation of new α-methylene-γ-lactone carbamates with NO production inhibitory effects in lipopolysaccharide-induced RAW 264.7 macrophages
- Author
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Wen-Hao Shao, Hu Yuan, Wei-Dong Zhang, Bing-Yang Chen, Ji Ye, Xiang-Rong Cheng, Wanlin Chang, Shan Lin, Hao Chen, and Qingyan Sun
- Subjects
Lipopolysaccharides ,Carbamate ,Lipopolysaccharide ,Stereochemistry ,medicine.medical_treatment ,Anti-Inflammatory Agents ,Chemistry Techniques, Synthetic ,Nitric Oxide ,Inhibitory postsynaptic potential ,Nitric oxide ,Lactones ,Mice ,chemistry.chemical_compound ,Drug Discovery ,medicine ,Animals ,Methylene ,Cytotoxicity ,IC50 ,Pharmacology ,chemistry.chemical_classification ,Macrophages ,Organic Chemistry ,General Medicine ,RAW 264.7 Cells ,chemistry ,Carbamates ,Lactone - Abstract
A series of new α-methylene-γ-lactone carbamates were synthesized by an asymmetric synthetic route. The activities on inhibiting nitric oxide (NO) release of these compounds were evaluated in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. The results indicated that most of the compounds except one exhibited potent NO inhibitory effect with IC50 value more than 2 μΜ. The cytotoxicities of these compounds were estimated via MTT assays. The results suggested that six compounds were accompanied by low cytotoxicity. The structure–activity relationships were also discussed. The S configuration of C3 on lactones ring would be more helpful to NO inhibitory effect.
- Published
- 2015