Short Synthesis of Molnupiravir (EIDD-2801) via a Thionated Uridine Intermediate [PDF]
Molnupiravir (MK-4482, EIDD-2801) is an experimental drug that has been demonstrated to be effective for the treatment of COVID-19 in human clinical trials. Herein, we report a concise synthesis of the drug via a novel thionated derivative that relies on one-pot methodologies, thus decreasing the number of purification steps required.
Somnath Yadav +2 more
exaly +6 more sources
EIDD-2801 resists to infection and co-infection of SARS-CoV-2 and influenza virus [PDF]
Background The coronavirus disease 2019 (COVID-19) pandemic has exerted a catastrophic impact on public health. Meanwhile, the seasonal influenza outbreak overlaps with the current pandemic wave.
Yuwei Gao, Beilei Shen
exaly +5 more sources
A High-Yielding Synthesis of EIDD-2801 from Uridine** [PDF]
A simple reordering of the reaction sequence allowed the improved synthesis of EIDD-2801, an antiviral with promising activity against the SARS-CoV-2 virus, starting from uridine. Compared to the original route, the yield was enhanced from 17% to 61%, and fewer isolation/purification steps were needed.
Sándor B Ötvös +2 more
exaly +5 more sources
Evaluation of molnupiravir (EIDD-2801) efficacy against SARS-CoV-2 in the rhesus macaque model [PDF]
Molnupiravir (EIDD-2801) is a prodrug of a ribonucleoside analogue that is currently being used under a US FDA emergency use authorization for the treatment of mild to moderate COVID-19. We evaluated molnupiravir for efficacy as an oral treatment in the rhesus macaque model of SARS-CoV-2 infection.
Dylan M Johnson +2 more
exaly +4 more sources
Preparing anti-SARS-CoV-2 agent EIDD-2801 by a practical and scalable approach, and quick evaluation via machine learning [PDF]
EIDD-2801 is an orally bioavailable prodrug, which will be applied for emergency use authorization from the U.S. Food and Drug Administration for the treatment of COVID-19.
Zhen Qin +7 more
doaj +4 more sources
SARS-CoV-2 infection is effectively treated and prevented by EIDD-2801 [PDF]
All known recently emerged human coronaviruses probably originated in bats1. Here we used a single experimental platform based on human lung-only mice (LoM) to demonstrate efficient in vivo replication of all recently emerged human coronaviruses (SARS-CoV, MERS-CoV and SARS-CoV-2) and two highly relevant endogenous pre-pandemic SARS-like bat ...
Kendra Gully +2 more
exaly +5 more sources
Molnupiravir and Its Active Form, EIDD-1931, Show Potent Antiviral Activity against Enterovirus Infections In Vitro and In Vivo [PDF]
Enterovirus infections can cause hand, foot, and mouth disease (HFDM), aseptic meningitis, encephalitis, myocarditis, and acute flaccid myelitis, leading to death of infants and young children.
Wu Zhong, Ruiyuan Cao, Qingsong Dai
exaly +4 more sources
Quantitative efficacy paradigms of the influenza clinical drug candidate EIDD-2801 in the ferret model [PDF]
Seasonal influenza viruses cause major morbidity and mortality worldwide, threatening in particular older adults and the immunocompromised. Two classes of influenza therapeutics dominate current disease management, but both are compromised by pre-existing or rapidly emerging viral resistance.
Jeong-Joong Yoon +2 more
exaly +5 more sources
Progress Toward a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine [PDF]
Grace P Ahlqvist +2 more
exaly +3 more sources
Progress Towards a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine [PDF]
Molnupiravir (MK-4482, EIDD-2801) is a promising orally bioavailable drug candidate for treatment of COVID-19. Herein we describe a supply-centered and chromatography-free synthesis of molnupiravir from cytidine, consisting of two steps: a selective enzymatic acylation followed by transamination to yield the final drug product.
Ahlqvist GP +8 more
europepmc +7 more sources

