Intravenous Peramivir as a Candidate for SARS-CoV-2 Antiviral Drug
Peramivir is a novel intravenous neuraminidase inhibitor (NAI), created by structure-based drug design (SBDD), consisting of a cyclopentane backbone with a positively charged guanidinyl group and lipophilic side chains. Creative Biolabs has established excellent platforms for drug development. We provide a variety of antiviral agents development services to meet the diverse needs of our customers.
The cyclopentane backbone on peramivir is somewhat similar to that of zanamivir and oseltamivir, but peramivir binds to the influenza neuraminidase with a much tighter binding affinity than oseltamivir carboxylate and has shown comparable or better neuraminidase-inhibiting activity than oseltamivir carboxylate. Peramivir mimics the sialic acid residues of the viral membrane and produces tight interactions with conserved residues of the neuraminidase active site competing with neuraminic acid for binding, thereby preventing the release of progeny virions from the infected host cell. Another important antiviral effect of peramivir is the inhibition of the passage of influenza virions through the mucosal layer of the respiratory epithelium.
Peramivir has a broad spectrum of activity against a wide range of influenza type A and B viruses. In addition, it also has potent antiviral effects against highly pathogenic and pandemic potential influenza virus subtypes H5N1 and H9N2 and inhibits the replication of nine types of avian influenza viruses. Peramivir has a favorable pharmacokinetic profile including high water solubility, low plasma protein binding, efficient renal clearance, and long serum half-life permitting once-daily intravenous dosing.
Fig.1 Design the structure of peramivir based on the SBDD method.
Once the crystal structure of influenza neuraminidase was solved, rational, SBDD method lead to several candidate NAIs, such as oseltamivir, zanamivir, and peramivir. Peramivir differs structurally from other NAIs through a novel substitution that results in multiple binding interactions with the active site and allows the antiviral to be active against some viruses that are resistant to other antivirals. Similarly, the structural information of the SARS-CoV-2 viruses has also established a solid structural basis for structure-based drug design for new-generation drugs. Creative Biolabs have derived optimized quantitative structure-activity relationship (QSAR) models with the purpose of proposing a presumable model for identifying effective inhibitors and designing new compounds. We can provide the SBDD methods for the development of new inhibitors used for SARS-CoV-2 treatment.
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