COVID-19 therapeutics: Small-molecule drug development targeting SARS-CoV-2 main protease
The severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) is the causative factor
behind the 2019 global coronavirus pandemic (COVID-19). The main protease, known as M …
behind the 2019 global coronavirus pandemic (COVID-19). The main protease, known as M …
SARS-CoV-2 main protease drug design, assay development, and drug resistance studies
Conspectus SARS-CoV-2 is the etiological pathogen of the COVID-19 pandemic, which led
to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The …
to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The …
Exploring diverse reactive warheads for the design of SARS-CoV-2 main protease inhibitors
Abstract SARS-CoV-2 main protease (M pro) is a validated antiviral drug target of
nirmatrelvir, the active ingredient in Pfizer's oral drug Paxlovid. Drug-drug interactions limit …
nirmatrelvir, the active ingredient in Pfizer's oral drug Paxlovid. Drug-drug interactions limit …
Fluorine-a small magic bullet atom in the drug development: perspective to FDA approved and COVID-19 recommended drugs
During the last twenty years, organic fluorination chemistry established itself as an important
tool to get a biologically active compound. This belief can be supported by the fact that every …
tool to get a biologically active compound. This belief can be supported by the fact that every …
Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome …
CS Dampalla, MJ Miller, Y Kim, A Zabiegala… - European Journal of …, 2023 - Elsevier
The high morbidity and mortality associated with SARS-CoV-2 infection, the etiological
agent of COVID-19, has had a major impact on global public health. Significant progress has …
agent of COVID-19, has had a major impact on global public health. Significant progress has …
Discovery and mechanism study of SARS-CoV-2 3c-like protease inhibitors with a new reactive group
P Ren, H Li, T Nie, X Jian, C Yu, J Li, H Su… - Journal of Medicinal …, 2023 - ACS Publications
3CLpro is an attractive target for the treatment of COVID-19. Using the scaffold hopping
strategy, we identified a potent inhibitor of 3CLpro (3a) that contains a thiocyanate moiety as …
strategy, we identified a potent inhibitor of 3CLpro (3a) that contains a thiocyanate moiety as …
Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors
A Wu, K Shi, J Wang, R Zhang, Y Wang - European Journal of Medicinal …, 2023 - Elsevier
The COVID-19 pandemic, caused by SARS-CoV-2, has had a huge impact on global health.
To respond to rapidly mutating viruses and to prepare for the next pandemic, there is an …
To respond to rapidly mutating viruses and to prepare for the next pandemic, there is an …
Structure-guided optimization of adenosine mimetics as selective and potent inhibitors of coronavirus nsp14 N7-methyltransferases
M Hausdorff, A Delpal, S Barelier, L Nicollet… - European Journal of …, 2023 - Elsevier
The COVID-19 pandemic reveals the urgent need to develop new therapeutics targeting the
SARS-CoV-2 replication machinery. The first antiviral drugs were nucleoside analogues …
SARS-CoV-2 replication machinery. The first antiviral drugs were nucleoside analogues …
Design of a SARS-CoV-2 papain-like protease inhibitor with antiviral efficacy in a mouse model
The emergence of SARS-CoV-2 variants and drug-resistant mutants calls for additional oral
antivirals. The SARS-CoV-2 papain-like protease (PLpro) is a promising but challenging …
antivirals. The SARS-CoV-2 papain-like protease (PLpro) is a promising but challenging …
Korupensamine A, but not its atropisomer, korupensamine B, inhibits SARS-CoV-2 in vitro by targeting its main protease (Mpro)
By combining docking and molecular dynamics simulations, we explored a library of 65
mostly axially chiral naphthylisoquinoline alkaloids and their analogues, with most different …
mostly axially chiral naphthylisoquinoline alkaloids and their analogues, with most different …