Sigut

Santiago’s Case Study: Antiviral Kit

April 5, 2022

Research in a time of COVID-19

When a thousand people worldwide suffered from lethal coronavirus (COVID-19) in 2020, we came up with an ambitious project to contribute to the worldwide pandemic solution.

Everything started with the question: How can we contribute as a small chemical company? Firstly, we thought about the distribution of anti-bacterial solutions, but this intention was unfortunately limited by Good manufacturing practice (GMP) for companies with a licence. Therefore, we turned out attention to the area that is closest to us and in which we excel, organic synthesis.

When the pandemic started, the hunt for an effective vaccine was launched simultaneously. Scientists from all over the world began their fight against a new type of coronavirus. First of all, the known potential drugs were re-purposed and tested. The most promising, which showed preliminary activity against COVID-19, were Remdesivir, Favipiravir, Chloroquine, Hydroxychloroquine, Azithromycin, etc. (Figure 1).

 

[caption id="attachment_18158" align="aligncenter" width="733"] Figure 1: Structures of the most promising drug candidates for treating COVID-19.[/caption]
 

Aviromix- antiviral drug candidate kit

We realized it was almost impossible to find a distributor that offers all of the most promising drug candidates for treating COVID-19. Moreover, the shipping times ranged from 1 to 4 weeks, which was unacceptable under this pandemic situation, where hundreds of people died every day. 

Our goal was the distribution of antiviral sets consisting of the five most potent and promising
re-purposed drugs in a short time. These sets were designed for institutes dealing with the synthesis of new promising drug candidates, virology labs, and microbiology labs to promote their effort. The significant advantages of this set were as follows:

1. quick delivery (within 48 h in EU)

2. all potential drugs at once, ready for use

3. extensive supporting information for each drug in the set

4. DNA free

5. easy to find on our new website

 

These sets (called Aviromix) may also serve as potential standards for the comparatition of newly invented drugs or as building blocks.

[caption id="attachment_18161" align="aligncenter" width="531"] Figure 2: Aviromix set.[/caption]

Remdesivir synthesis

During only three months, starting from January 2020, we optimized the total multigram scaled synthesis of Remdesivir in our lab (Figure 2). The rest of the drug candidates were purchased, dosed into the sets and irradiated to destroy all present DNA. All the missing analytical information was completed, and if necessary further purification was undergone. We also created a new website for convenient and quick purchases for our future customers.

If you want to read more about our research of antiviral nucleoside prodrugs such as Remdesivir, you can find our article published previously here.

[caption id="attachment_18162" align="aligncenter" width="506"] Figure 3: Scale-up of Remdesivir intermediate.[/caption]

And what happened next?

Since we were already successful with the synthesis of Remdesivir, we turned our attention to Remdesivir metabolites, mono-, di- and triphosphate. To this day we have sold these Remdesivir phosphates to tens of clients worldwide. 

 

Finally, with gaining experience in the field of antiviral compounds, we have advanced our research to the development of novel nucleoside triphosphates with biological activity. You can read more about this research here

 


For the realization of this project, we would like to thank MPO (Ministry of industry and trade) and SIC (Central Bohemian innovation centre) for the financial support.

If you want to discover more about our services, discuss specific research, or receive a proposal, please do not hesitate to write an email to Krystof Sigut at krystof.sigut@santiago-lab.com or reach him on the phone +420 776 750 591.

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