期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 18, 页码 8402-8416出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00931
关键词
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资金
- Centre National de la Recherche Scientifique
- Aix-Marseille Universite
Rhinoviruses (RVs) have been linked to exacerbations of many pulmonary diseases, thus increasing morbidity and/or mortality in subjects at risk. Unfortunately, the wide variety of RV genotypes constitutes a major hindrance for the development of Rhinovirus replication inhibitors. In the current investigation, we have developed a novel series of pyrazole derivatives that potently inhibit the Rhinovirus replication. Compounds 10e and 10h behave as early stage inhibitors of Rhinovirus infection with a broad-spectrum activity against RV-A and RV-B species (EC50 < 0.1 mu M). We also evaluate the dynamics of the emerging resistance of these promising compounds and their in vitro genotoxicity. Molecular docking experiments shed light on the pharmacophoric elements interacting with residues of the drug-binding pocket.
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