Middle East respiratory syndrome coronavirus (MERS-CoV) has been one of the scariest disease owing to its mortality and possibility of global outbreak. Until July 2019, a total of 2458 laboratory-confirmed cases of MERS, including 848 associated deaths (case-fatality rate: 34.5%) were globally reported from 27 countries. The MERS-CoV is the genus of Betacoronavirus in the family Coronaviridae. Coronaviruses are a group of positive-sense, single-stranded RNA viruses. The transmission of MERS-CoV is suspected through the respiratory secretions, such as coughing of an infected person. There is currently no effective vaccine or therapy available to prevent or treat infection with MERS-CoV. However, several fundamental and clinical studies have been completed or are underway. We screened 200,000 compounds of Korean Chemical Bank (KCB) against MERS-CoV using high content screening (HCS) platform of Institut Pasteur Korea (IPK). We found that 6-amino-4-anilino-quinazoline families were effective for inhibiting MERS-CoV infection. Quinazoline derivatives have previously been effective for inhibiting MERS-CoV infection. Quinazoline derivatives have previously been reported as potent inhibitors of the protein kinase of epidermal growth factor receptor (EGFR). Most of those compounds were approved as anticancer drugs, including Gefitinib, Lapatinib, Erlotinib, and Afatinib. We thought that quinazoline compounds can exhibit good bioavailability and be easily extended to treatment of MERS-CoV infection. This presentation will discuss the synthesis and biological effects of 4-anilino-quinazoline derivatives.

Discovery of novel 4-anilinoquinazoline derivatives as potent MERS-CoV inhibitors

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.