Beilstein J. Org. Chem.2013,9, 197–203, doi:10.3762/bjoc.9.23
compound from this series for development, we sought to increase both the potency and the aqueous solubility of 1. Lead optimization has achieved compounds with potent antiviral activity against a panel of myxovirus family members (EC50 values in the low nanomolar range) and much improved aqueous
: asymmetric synthesis; benzimidazole; host-directed; myxovirus; small molecule inhibitor; Introduction
Myxoviruses are divided into two evolutionarily distinct yet related families: the orthomyxoviridae, which is composed largely of the influenza viruses, and the paramyxoviridae, which includes respiratory
principle, less susceptibility to the development of resistance.
Using high-throughput screening, in combination with counter-screening for detecting a broadened viral target spectrum that extends to other pathogens of the myxovirus families, our research group has been successful in identifying small
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Graphical Abstract
Figure 1:
Structure of first-generation lead compound 1.