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. 2023 Nov 15:260:115760.
doi: 10.1016/j.ejmech.2023.115760. Epub 2023 Aug 28.

Synthesis of cannabidiol-based compounds as ACE2 inhibitors with potential application in the treatment of COVID-19

Gabriel Vitor de Lima Marques  1 , Daisymara Priscila de Almeida Marques  2 , Felipe Alves Clarindo  2 , Jesus Alberto Avendaño-Villarreal  3 , Fabiana Sélos Guerra  4 , Patrícia Dias Fernandes  4 , Eduardo Nicolau Dos Santos  3 , Elena Vitalievna Gusevskaya  3 , Markus Kohlhoff  5 , Fabrício de Araújo Moreira  6 , Luis Adan Flores Andrade  7 , Flávio Guimarães da Fonseca  7 , Jordana Grazziela Alves Coelho Dos-Reis  2 , Renata Barbosa de Oliveira  8
Affiliations

Synthesis of cannabidiol-based compounds as ACE2 inhibitors with potential application in the treatment of COVID-19

Gabriel Vitor de Lima Marques et al. Eur J Med Chem. .

Abstract

Cannabis is a general name for plants of the genus Cannabis. Used as fiber, medicine, drug, for religious, therapeutic, and hedonistic purposes along the millenia, it is mostly known for its psychoactive properties. One of its major constituents, cannabidiol (CBD), a non-psychoactive substance, among many other biological activities, has shown potential as an anti-SARS-CoV-2 drug. In this work, three derivatives and an analogue of CBD were synthesized, and cell viability and antiviral activities were evaluated. None of the compounds showed cytotoxicity up to a maximum concentration of 100 μM and, in contrast, displayed a significant antiviral activity, superior to remdesivir and nafamostat mesylate, with IC50 values ranging from 9.4 to 1.9 μM. In order to search for a possible molecular target, the inhibitory activity of the compounds against ACE2 was investigated, with expressive results (IC50 ranging from 3.96 μM to 0.01 μM).

Keywords: ACE2 inhibitors; COVID-19; Cannabidiol derivatives; SARS-CoV-2.

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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