期刊论文

Wan, Jian

英文

Bioorganic & Medicinal Chemistry

0968-0896

2015

23

7

1395-1401

10.1016/j.bmc.2015.02.047

In summary, a series of newly 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives 3 were prepared as potential E. coli PDHc-E1 inhibitors and their antifungal activity was evaluated. All tested compound 3 exhibited significant inhibition against E. coli PDHc-E1 (IC50 <21 μM). Compound 3g was found to be the most powerful inhibitor (IC50 = 4.21 ± 0.11) and was recognized to act as a competitive inhibitor of ThDP against E. coli PDHc-E1 by the kinetic analysis. Compounds 3g, 3n, 3p, and lead compound I-

本校为第一且通讯机构

To identify new antifungal lead compound based on inhibitors of pyruvate dehydrogenase complex E1, a series of 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives 3 were prepared and evaluated for their Escherichia coli PDHc-E1 inhibitory activity and antifungal activity. The in vitro bioassay for the PDHc-E1 inhibition indicated all the compounds exhibited significant inhibition against E. coli PDHc-E1 (IC50 < 21 mu M), special compound 3g showed the most potent inhibitory activity (IC50 = 4.21 +/- 0.11 mu M) and was demonstrated to act as a competitive inhibitor of PDHc-E1. Meanwhile, inhibi...