2. Academic Validation
  3. The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

  • Bioorg Med Chem Lett. 2007 Mar 15;17(6):1812-7. doi: 10.1016/j.bmcl.2006.12.038.
Pei-Wen Hsieh 1,  Tsong-Long Hwang,  Chin-Chung Wu,  Shin-Zan Chiang,  Chung-I Wu,  Yang-Chang Wu
Affiliations

Affiliation

  • 1 Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
PMID: 17197180 DOI: 10.1016/j.bmcl.2006.12.038
Abstract

Forty-seven 2-benzoylaminobenzoic esters were synthesized and evaluated in anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil Elastase release assays. Most 2-benzoylamino-4-chlorobenzoic acid derivatives showed selective inhibitory effects on arachidonic acid (AA)-induced platelet aggregation. Among them, compounds 6b and 7b exhibited more potent inhibitory effects (CA. 200-fold) than aspirin. Additionally, compounds 1a and 5a showed strong inhibitory effects on neutrophil superoxide generation with IC(50) values of 0.65 and 0.17 microM, respectively. However, compounds 6d and 6e exhibited dual inhibitory effects on platelet aggregation and neutrophil Elastase (NE) release; therefore, these two compounds may be new leads for development as anti-inflammatory and anti-platelet aggregatory agents.

Figures