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  • Title: [Synthesis and anti-inflammatory activity of alpha-substituted p-(methanesulfonyl)phenylpropenamides].
    Author: Ao GZ, Zhang YH, Ji H, Deng G.
    Journal: Yao Xue Xue Bao; 2003 Sep; 38(9):671-6. PubMed ID: 14730916.
    Abstract:
    AIM: To search for new compounds with strong anti-inflammatory activity and low gastrointestinal (GI) side effects. METHODS: A series of alpha-substituted p-(methanesulfonyl) phenyl-propenamides were synthesized. Their anti-inflammatory activities against xylene-induced mice ear swelling and carrageenan-induced rat paw edema were evaluated, and their GI side effects in rats were examined. RESULTS: Twenty-five target compounds (II1-25) were obtained, and their structures were determined by IR, 1H NMR, MS and elemental analysis. Thirteen compounds (II1,3,5,8-13,15,18,19,23) exhibited marked anti-inflammatory activity comparable to diclofenac sodium (DC) and rofecoxib (RC) in xylene-induced mice ear swelling model, and twelve compounds (II1,3,5,7,8,10-12,17,18,20,23) showed remarkable anti-inflammatory activity comparable to DC and RC in carrageenan-induced rat paw edema. Compounds II3,8,10,11,18,20 showed GI side effects less than DC (P < 0.01), and no significant difference compared with RC and CMC-Na (P > 0.05). CONCLUSION: alpha-Substituted p-(methanesulfonyl)phenylpropenamides showed strong anti-inflammatory activity but few GI side effects and deserve to be further investigated.
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