Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.

ABSTRACT: A selection of compounds from a proprietary library, based on chemical diversity and various biological activities, was evaluated as potential inhibitors of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) in a phenotypic-based screening assay. A compound based on a 2-phenylquinoline scaffold emerged as the most promising hit, with EC₅₀ and CC₅₀ values of 6 and 18 μM, respectively. The subsequent selection of additional analogues, along with the synthesis of ad hoc derivatives, led to compounds that maintained low μM activity as inhibitors of SARS-CoV-2 replication and lacked cytotoxicity at 100 μM. In addition, the most promising congeners also show pronounced antiviral activity against the human coronaviruses HCoV-229E and HCoV-OC43, with EC_50</

SUBMITTER: Nizi MG 

PROVIDER: S-EPMC9088073 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature