| Title | Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors. | ||
| Author | Im, Isak; Lee, Eui Seung; Choi, Soo Jeong; Lee, Ju-Yeon; Kim, Yong-Chul | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 2009-Jul |
| PMID | 19464175 | PMCID | PMC7126291 |
| Affiliation | 1.Research Center for Biomolecular Nanotechnology, Department of Life Science, Gwangju Institute of Science and Technology, Republic of Korea. | ||
Human rhinovirus 3C protease (HRV 3C(pro)) is known to be a promising target for development of therapeutic agents against the common cold because of the importance of the protease in viral replication as well as its expression in a large number of serotypes. To explore non-peptidic inhibitors of HRV 3C(pro), a series of novel heteroaromatic esters was synthesized and evaluated for inhibitory activity against HRV 3C(pro), to determine the structure-activity relationships. The most potent inhibitor, 7, with a 5-bromopyridinyl group, had an IC(50) value of 80nM. In addition, the binding mode of a novel analog, 19, with the 4-hydroxyquinolinone moiety, was explored by molecular docking, suggesting a new interaction in the S1 pocket.