Novel small-molecules using alkyne groups to inhibit the SARS-CoV-2 main protease.
New antiviral for the treatment of COVID-19.
Selective irreversible covalent reaction of viral main proteases and other nucleophilic cysteine proteases.
Alkynes are substantially less reactive towards reaction with nucleophiles than most other functional groups, enhancing selectivity for target inhibition versus off target inhibition.
Alkyne bearing small-molecules less likely to interfere with host proteins.
Highly desired from a drug safety perspective.
Alkynes can be functionalised at their terminal position.
Optimises inhibition and selectivity, including with respect to drug-resistant Mpro variants, as well as their pharmacodynamic and pharmacokinetic properties.
Demonstrated inhibition of other related viral, bacterial, and human proteases.
Potential for treatment of other viral infections, such as with middle eastern