The 3D-QSAR study of non-peptide bradykinin antagonists by CoMFA

Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. Some active compounds such as FR 173657, LF 160687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed and synthesized the iminodiacetic acid derivatives having two or three amide bonds and lipophilic ring system in each molecule. Liquid phase combinatorial synthesis using the iminodiacetic acid template gave diverse individual compounds rapidly and efficiently on a 10-50 mg scale. (omitted)