Discussions

Oseltamivir for SARS-CoV-2 has demonstrated effectiveness in treating and preventing influenza virus infections that occur spontaneously. Oseltamivir was created with two main discoveries in mind. First off, it was previously established that the transition-state analog 2,3-dehydro-2-deoxy-N-acetylneuraminic acid (DANA) was a modest neuraminidase inhibitor. Second, a vacant negatively charged pocket in the vicinity of the C4 on the sugar ring was discovered by analyzing the structure of the sialic acid substrate in association with the enzyme active site. This implied that better affinity binding might result from replacing the C4-OH with a bigger basic residue. When a 4-guanidino group was substituted for the C4-OH, the binding was increased over 10,000 times above DANA.