Therapeutic strategies for COVID-19: progress and lessons learned

G Li, R Hilgenfeld, R Whitley, E De Clercq - Nature Reviews Drug …, 2023 - nature.com
Abstract The coronavirus disease 2019 (COVID-19) pandemic has stimulated tremendous
efforts to develop therapeutic strategies that target severe acute respiratory syndrome …

Recent advances in SARS-CoV-2 main protease inhibitors: from nirmatrelvir to future perspectives

A Citarella, A Dimasi, D Moi, D Passarella, A Scala… - Biomolecules, 2023 - mdpi.com
The main protease (Mpro) plays a pivotal role in the replication of severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2) and is considered a highly conserved viral target …

Fluorine-a small magic bullet atom in the drug development: perspective to FDA approved and COVID-19 recommended drugs

G Chandra, DV Singh, GK Mahato, S Patel - Chemical Papers, 2023 - Springer
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 …

Alkyne as a Latent Warhead to Covalently Target SARS-CoV-2 Main Protease

C Ngo, W Fried, S Aliyari, J Feng, C Qin… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need for improved therapy to better control the ongoing COVID-19
pandemic. The main protease Mpro plays a pivotal role in SARS-CoV-2 replications, thereby …

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 …

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

αβ, α′ β′-Diepoxyketones are mechanism-based inhibitors of nucleophilic cysteine enzymes

M de Munnik, J Lithgow, L Brewitz… - Chemical …, 2023 - pubs.rsc.org
Epoxides are an established class of electrophilic alkylating agents that react with
nucleophilic protein residues. We report αβ, α′ β′-diepoxyketones (DEKs) as a new type …

On the origins of SARS-CoV-2 main protease inhibitors

YL Janin - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
In order to address the world-wide health challenge caused by the COVID-19 pandemic, the
3CL protease/SARS-CoV-2 main protease (SARS-CoV-2-Mpro) coded by its nsp5 gene …

Covalent small-molecule inhibitors of SARS-CoV-2 Mpro: Insights into their design, classification, biological activity, and binding interactions

AM Shawky, FA Almalki, HA Alzahrani… - European Journal of …, 2024 - Elsevier
Since 2020, many compounds have been investigated for their potential use in the treatment
of SARS-CoV-2 infection. Among these agents, a huge number of natural products and FDA …

Discovery of Orally Available and Brain Penetrant AEP Inhibitors

D Krummenacher, W He, B Kuhn… - Journal of Medicinal …, 2023 - ACS Publications
Alzheimer's Disease (AD) is the most widespread form of dementia, with one of the
pathological hallmarks being the formation of neurofibrillary tangles (NFTs). These tangles …