Acyclovir Fleximer for the Treatment of SARS-CoV-2

Creative Biolabs is a leading service provider that focuses on acyclovir fleximer nucleoside analogues development services for the treatment of 2019 Novel Coronavirus (SARS-CoV-2). Creative Biolabs offers advanced drug discovery solutions in an efficient and cost-effective way for global customers. Based on our top technology platform, our experienced scientists will work with you at each step of your programs and get the results you need to make critical decisions and advance your projects.

Introdiction of SARS-CoV-2

SARS-CoV-2, a new strain of coronavirus identified in 2019, has not been found in humans previously. SARS-CoV-2 is different from both MERS-CoV and SARS-CoV, and it is the seventh member of the family of coronaviruses that infect humans. Until now, there are no approved treatments or vaccines for human coronaviruses (HCoVs) or potentially lethal zoonotic CoVs, including Middle East respiratory syndrome (MERS), severe acute respiratory syndrome (SARS), and SARS-CoV-2. SARS-CoV was first identified in 2002 and it is a new coronavirus pathogen causing severe lung disease, and before the end of the outbreak, over 8,000 cases were confirmed in a variety of countries, leading to about 812 fatalities. MERS-CoV was identified in 2012, it is a second zoonotic coronavirus that can result in lethal respiratory infections in humans and caused many people died. Hence, there is a great need for novel and more effective antiviral therapeutics, especially those targeting emerging and reemerging infectious diseases and pathogens.

Coronavirus.

Acyclovir Fleximer

Fleximers are different series of flexible, or “split” purine base analogues designed to learn how nucleobase flexibility affects the recognition, binding, and activity of nucleoside(tide) analogues. There is a purine base scaffold in the fleximers. With this purine base scaffold, the imidazole and pyrimidine moieties are combined by a single carbon-carbon bond, rather than being “fused” as is typical for the purines.

In previous reports, a number of novel fleximers have been screened, and these fleximers can combine the flex-base motif with the flexible acyclic sugar scaffold of the FDA-approved drug acyclovir (serves as a polymerase inhibitor). Studies demonstrated that these fleximers can inhibit HCoV-NL63 and MERS-CoV replication in cell culture. However, it is still unknown how these novel analogues disrupt viral replication. In summary, acyclovir fleximers are a group of promising drug candidates for the new drug discovery of SARS-CoV-2.

Acyclovir (ACV) and target fleximer analogues (1–3). Fig.1 Acyclovir (ACV) and target fleximer analogues (1–3).

Drug Discovery Services at Creative Biolabs

As a forward-looking drug discovery service provider, Creative Biolabs has built a one-stop drug discovery platform. With our advanced techniques, we can provide design, screening, synthesis and validation services of acyclovir fleximer to support our clients’ drug discovery project for SARS-CoV-2.

Our drug discovery services include but not limited to:

  • Target identification and validation
  • Hit identification
  • Hit to lead
  • Lead optimization
  • IND-Enabling

Creative Biolabs will continue to advance technologies and techniques in parallel to ensure the success for customers worldwide. Please directly contact us with your project request for more details.

Reference

  1. Hannah, L.P.; et al. Design, synthesis and evaluation of a series of acyclic fleximer nucleoside analogues with anti-coronavirus activity. Bioorg Med Chem Lett. 2015, 25(15): 2923–2926
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