Design, synthesis and antiinflammatory activity of novel phthalimide derivatives, structurally related to thalidomide
作者:Alexandre Légora Machado、Lı́dia Moreira Lima、João Xavier Araújo-Jr、Carlos Alberto M. Fraga、Vera Lúcia Gonçalves Koatz、Eliezer J. Barreiro
DOI:10.1016/j.bmcl.2004.12.012
日期:2005.2
As part of an ongoing effort to develop new thalidomide analogues as antiinflammatory lead-candidates, this paper describes the synthesis and antiinflammatory activity of novel N-phenyl-phthalimide functionalized derivatives (4a-d, 5a,b, 6a,b). The target compounds were assayed in an acute lung inflammatory model and all compounds were able to inhibit TNF-alpha production and subsequent neutrophil
作为开发新的沙利度胺类似物作为抗炎先导候选药物的持续努力的一部分,本文描述了新型N-苯基-邻苯二甲酰亚胺官能化衍生物(4a-d,5a,b,6a,b)的合成和抗炎活性。在急性肺炎模型中测定了目标化合物,并且所有化合物均能够在LPS急性肺炎模型中抑制TNF-α的产生和随后的中性粒细胞募集。