The Organic and Medical Chemistry group of the UJI is working on the development of new antiviral molecules against COVID-19



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## The Organic and Medical Chemistry group of the UJI is working on the development of new antiviral molecules against COVID-19

21/05/2020 |
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Researchers from the Organic and Medical Chemistry group at the Universitat Jaume I (OrgMedChem), coordinated by Florenci González Adelantado, are working on the development of new antiviral molecules against SARS-CoV-2. Specifically, the aim of the project is to have specific cysteine protease inhibitors for SARS-CoV-2 proteases that will serve as innovative therapy against COVID-19.

The OrgMedChem group has been working for years on the development of cysteine protease inhibitors that have proven to be very potent in vitro against parasitic cysteine proteases. In this line, two cysteine proteases have been identified in SARS-CoV-2 as therapeutic targets, so the aim is to adapt the chemical synthesis of these inhibitors already developed in order to prepare new molecules that are more selective for the virus targets and with a pharmacokinetics (process through which a drug passes from the moment it is administered until its total elimination from the body) suitable for COVID-19.

In the first phase of the project, it will be tested in vitro with the inhibitors already developed by the group to observe their response. On the basis of these results, new inhibitors with similar characteristics, but more specific to SARS-CoV-2, can be synthesised so that the tests can be carried out and subsequently used as a drug if they are effective.

Protease inhibitors have proven to be a valid tool for fighting the virus, as they were in the case of AIDS. However, proteases are very diverse for each type of virus, so it is necessary to use active, targeted inhibitors for SARS-CoV-2's own proteases, thus increasing the effectiveness of therapy. 

The two SARS-CoV-2 proteases are both cysteine proteases, although they are different: "3CLpro" is a chymotrypsin-type protease, while "PLpro" belongs to the papain family. Very recently, the X-ray structure of the SARS-CoV-2 protease "3CLpro" has been published and also protease inhibitors are under development. The proposal of the Universitat Jaume I group represents the implementation of more specific inhibitors of the papain family (PLpro), the second protease of SARS-CoV-2.

It is important to emphasise that SARS-CoV-2 shares 82% of sequence with SARS-CoV virus and more than 90% in some essential enzymes, so relations between both can be established. Numerous studies show that cysteine protease inhibitors block the replication of the SARS-CoV virus up to the nanomolar order and indicate that other proteases such as cathepsins B and L could be involved in the viral invasion process. In this sense, the OrgMedChem group has published and patented small molecules that act as selective and powerful inactivators of cysteine proteases of the papain family that are found in protozoa causing infectious diseases and human cathepsins B and L. 

Thus, the project "Cysteine protease inhibitors against SARS-CoV-2" starts from the previous works of the group with cysteine protease inhibitors as potential drugs against infectious diseases in which a cysteine protease-type enzyme belonging to the papain family has been identified. These infectious diseases include tropical infectious diseases caused by protozoa, but also diseases caused by viruses. Specifically, the group has tested inhibitors against the *Trypanosomabrucei* parasites that cause human African trypanosomiasis, against *Trypanosomacruzi* that causes Chagas disease, or against *Plasmodiumfalciparum* that causes malaria. Some inhibitors have also been tested against *Leishmaniadonovanii*, which causes kala-azar, also called *visceral leishmaniasis*. 

The new inhibitors to be developed for SARS-CoV-2 cysteine proteases will be based on these previously developed inhibitors which proved to be very active, but adapted appropriately to increase affinity with the corresponding enzymes. In addition, the new molecules will be subjected to previous computational studies by the group of lecturer Vicent Moliner of the UJI thanks to the availability of the X-ray structures of the recently published "3CLpro" and "PLpro" of SARS-COV-2.

Articles:

[Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates](http://dx.doi.org/10.1016/j.bmc.2018.07.015). BIOORGANIC & MEDICINAL CHEMISTRY. Num. 16. Vol. 26. pp. 4624-4634. 2018. 

[Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain](http://dx.doi.org/10.1021/acsmedchemlett.6b00276). ACS Medicinal Chemistry Letters. Num. 12. Vol. 7. pp. 1073-1076. 2016. 

[Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic traps](http://dx.doi.org/10.1021/acs.joc.5b01013). JOURNAL OF ORGANIC CHEMISTRY. Num. 5. Vol. 80. pp. 7752-7756. 2015. 

[Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action](http://dx.doi.org/10.1002/cmdc.201500204). CHEMMEDCHEM. Num. 9. Vol. 10. pp. 1484-1487. 2015. 

[Dipeptidyl-a,b-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain](http://dx.doi.org/10.1016/j.bmcl.2007.10.056). BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. Num. 24. Vol. 17. pp. 6697-6700. 2007.

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