Antiviral compounds targeting the 3CL protease of the porcine epidemic diarrhea virus (PEDV)

Coumarin-based therapeutic agent for porcine epidemic diarrhea that inhibits PEDV 3CL protease

This technology is a composition for the prevention and treatment of porcine epidemic diarrhea (PED) that uses two bicoumarin-based furancarboxylate compounds as active ingredients, which bind to the 3CL protease essential for the replication of the PED virus. It is designed for use not only as a pharmaceutical but also as an animal drug, feed additive, drinking water additive, and natural disinfectant.

Porcine epidemic diarrhea is caused by the coronavirus PEDV, which can lead to a mortality rate of nearly 100% in infected piglets. It has caused massive losses for pig farms, including the death of approximately 8 million pigs in the U.S. alone between 2013 and 2014. Commercially available inactivated and attenuated vaccines have not provided sufficient protection against variant viruses, and no antiviral drugs capable of directly treating the disease had been developed until now.

This technology identifies compounds from a natural compound database that exhibit excellent binding affinity and stability with 3CL protease, a key enzyme for viral protein degradation, thereby inhibiting viral replication. It adapts the protease inhibitor strategy proven effective in treating HIV and Hepatitis C for use in swine diseases. Applicable to animal drugs, feed and drinking water additives for piglets in farrowing houses, and barn disinfectants, it helps reduce piglet mortality during outbreaks of variant PEDV that are difficult to control with vaccines alone, providing a means to block farm-level spread.

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Key Features:

• Active ingredient comprising the compound ZINC04339983, 2-oxo-4-(2-oxochromen-3-yl)chromen-7-yl furan-2-carboxylate, or a pharmaceutically acceptable salt thereof
• Active ingredient comprising the compound ZINC09517238, 4-(8-methoxy-2-oxo-chromen-3-yl)-2-oxo-chromen-7-yl furan-2-carboxylate, or a pharmaceutically acceptable salt thereof
• Pharmaceutical composition for the prevention or treatment of porcine epidemic diarrhea that inhibits viral replication by targeting the 3CL protease of the porcine epidemic diarrhea virus
• Feed additives, drinking water additives, and natural disinfectants for the prevention or improvement of porcine epidemic diarrhea containing the compound or its salt as an active ingredient

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This invention was developed with support from the Ministry of Agriculture, Food and Rural Affairs for the advancement and commercialization of PRRSV and PEDV antiviral agents.

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