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2020 ; 25
(10
): ä Nephropedia Template TP
gab.com Text
Twit Text FOAVip
Twit Text #
English Wikipedia
Comparative Antiviral Activity of Remdesivir and Anti-HIV Nucleoside Analogs
Against Human Coronavirus 229E (HCoV-229E)
#MMPMID32429580
Parang K
; El-Sayed NS
; Kazeminy AJ
; Tiwari RK
Molecules
2020[May]; 25
(10
): ä PMID32429580
show ga
Remdesivir is a nucleotide prodrug that is currently undergoing extensive
clinical trials for the treatment of COVID-19. The prodrug is metabolized to its
active triphosphate form and interferes with the action of RNA-dependent RNA
polymerase of SARS-COV-2. Herein, we report the antiviral activity of remdesivir
against human coronavirus 229E (HCoV-229E) compared to known anti-HIV agents.
These agents included tenofovir (TFV), 4'-ethynyl-2-fluoro-2'-deoxyadenosine
(EFdA), alovudine (FLT), lamivudine (3TC), and emtricitabine (FTC), known as
nucleoside reverse-transcriptase inhibitors (NRTIs), and a number of 5'-O-fatty
acylated anti-HIV nucleoside conjugates. The anti-HIV nucleosides interfere with
HIV RNA-dependent DNA polymerase and/or act as chain terminators. Normal human
fibroblast lung cells (MRC-5) were used to determine the cytotoxicity of the
compounds. The study revealed that remdesivir exhibited an EC(50) value of 0.07
µM against HCoV-229E with TC(50) of > 2.00 µM against MRC-5 cells. Parent NRTIs
were found to be inactive against (HCoV-229E) at tested concentrations. Among all
the NRTIs and 5'-O-fatty acyl conjugates of NRTIs, 5'-O-tetradecanoyl ester
conjugate of FTC showed modest activity with EC(50) and TC(50) values of 72.8 µM
and 87.5 µM, respectively. These data can be used for the design of potential
compounds against other coronaviruses.