4.6 Article

A sustainable synthesis of the SARS-CoV-2 Mpro inhibitor nirmatrelvir, the active ingredient in Paxlovid

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Business

Economic effects of the COVID-19 pandemic on entrepreneurship and small businesses

Maksim Belitski et al.

Summary: Responding to COVID-19 involves supporting small business jobs, creating productive entrepreneurship, and examining the role of financial mechanisms. The pandemic brings both challenges and opportunities for small businesses, highlighting the need for research on digitalization and financial support policies during crises.

SMALL BUSINESS ECONOMICS (2022)

Article Medicine, General & Internal

Molnupiravir for Oral Treatment of Covid-19 in Nonhospitalized Patients

A. Jayk Bernal et al.

Summary: This study found that early treatment with molnupiravir reduced the risk of hospitalization or death in at-risk, unvaccinated adults with Covid-19.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

Article Medicine, General & Internal

Oral Nirmatrelvir for High-Risk, Nonhospitalized Adults with Covid-19

Jennifer Hammond et al.

Summary: In high-risk, unvaccinated adults, treatment of Covid-19 with nirmatrelvir plus ritonavir can significantly reduce the risk of hospitalization and death, with good safety profile.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

Article Pharmacology & Pharmacy

Nirmatrelvir Plus Ritonavir: First Approval

Yvette N. Lamb

Summary: Nirmatrelvir plus ritonavir is a medication developed for the treatment and post-exposure prophylaxis of COVID-19. It received authorization in the UK and EU for use in adults at high risk for severe COVID-19. Nirmatrelvir is an inhibitor of SARS-CoV-2 main protease, while ritonavir is a protease inhibitor and CYP3A inhibitor.
Article Chemistry, Medicinal

Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CLProtease Inhibitor Clinical Candidate for Treating COVID-19

Yuto Unoh et al.

Summary: S-217622 is the first oral noncovalent, nonpeptidic SARS-CoV-2 3CL protease inhibitor clinical candidate, which could be a potential oral agent for treating COVID-19.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Organic

Environmentally Responsible and Cost-Effective Synthesis of the Antimalarial Drug Pyronaridine

Joseph R. A. Kincaid et al.

Summary: Two routes to synthesizing the antimalarial drug Pyronaridine are described, one with a linear sequence and the other with a convergent sequence. The overall yields of Pyronaridine are 87% and 95% respectively. Compared to existing methods using organic solvents, these routes reduce the environmental impact by a factor of 5 as measured by E Factors.

ORGANIC LETTERS (2022)

Review Pharmacology & Pharmacy

COVID-19 and the promise of small molecule therapeutics: Are there lessons to be learnt?

Wei Shen Ho et al.

Summary: This review analyzes the merits and limitations of drugs tested against SARS-CoV-2 and used for adjuvant therapy. Although many of these drugs have been proven ineffective, important lessons can be learned. The recent inclusion of molnupiravir and PaxlovidTM as treatment options for COVID-19 represents our best hope to date for living with COVID-19.

PHARMACOLOGICAL RESEARCH (2022)

Review Multidisciplinary Sciences

Stopping pandemics before they start: Lessons learned from SARS-CoV-2

Aled M. Edwards et al.

Summary: This article discusses the remarkable effectiveness of vaccine and drug responses to COVID-19, emphasizing the importance of long-term investment in technology and basic science. It also highlights the ongoing global pandemic and recommends proactive measures to prepare for, minimize the impact of, and prevent future pandemics.

SCIENCE (2022)

Article Chemistry, Multidisciplinary

An environmentally responsible synthesis of the antitumor agent lapatinib (Tykerb)

Julie Yu et al.

Summary: A greener synthesis route has been developed for the targeted antitumor agent, using a 5-step, 3-pot sequence mainly in recyclable water with only 500 ppm of a Pd catalyst, highlighting the reduction in catalyst usage compared to existing literature.

GREEN CHEMISTRY (2022)

Article Chemistry, Multidisciplinary

Dehydration of primary amides to nitriles in water. Late-stage functionalization and 1-pot multistep chemoenzymatic processes under micellar catalysis conditions

Alex B. Wood et al.

Summary: Dehydration of primary amides to nitriles can be achieved in aqueous micelles without the need for large amounts of organic co-solvents. A range of substrates, including functionalized molecules, can be converted using a sacrificial and inexpensive nitrile that can accept one equivalent of water. Catalyst loadings as low as 0.2-0.8 mol% of Pd(OAc)2 are possible in this recyclable medium with very low E Factors. This method is also applicable to one-pot reactions and chemoenzymatic catalysis, showcasing the benefits of chemistry in water.

GREEN CHEMISTRY (2022)

Article Chemistry, Organic

Time Economy in Total Synthesis

Yujiro Hayashi

Summary: This article highlights the importance of time economy in chemical synthesis and the general considerations for the rapid production of desired molecules. Through modern strategies and technologies, important drugs such as Tamiflu and ibuprofen can now be synthesized in a short period of time.

JOURNAL OF ORGANIC CHEMISTRY (2021)

Review Chemistry, Multidisciplinary

In Pursuit of Synthetic Efficiency: Convergent Approaches

Yang Gao et al.

Summary: The field of total synthesis has shifted its focus towards synthetic efficiency, with the convergent strategy being recognized as an effective approach. This strategy involves coupling fragments with similar complexity to efficiently synthesize target molecules. By employing innovative strategies and methodologies, efficient syntheses of complex molecules have been achieved in various chemical families.

ACCOUNTS OF CHEMICAL RESEARCH (2021)

Article Chemistry, Multidisciplinary

Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity

Chunlong Ma et al.

Summary: This study introduces a rational design of covalent SARS-CoV-2 M-pro inhibitors with novel cysteine reactive warheads, demonstrating potent enzymatic inhibition, antiviral activity, and improved target specificity compared to existing compounds. The promising lead candidates exhibit high selectivity over host proteases and are valuable chemical probes for target validation and potential drug development against SARS-CoV-2.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

Article Multidisciplinary Sciences

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

Dafydd R. Owen et al.

Summary: PF-07321332, an orally bioavailable SARS-CoV-2 main protease inhibitor, has been discovered with in vitro pan-human coronavirus antiviral activity and excellent off-target selectivity and in vivo safety profiles. This new drug has shown promise in countering the threat of COVID-19 with its oral activity and safety in clinical trials.

SCIENCE (2021)

Article Multidisciplinary Sciences

Efficacy of GC-376 against SARS-CoV-2 virus infection in the K18 hACE2 transgenic mouse model

C. Joaquin Caceres et al.

Summary: GC-376 treatment showed slight improvement in survival in mice challenged with a high virus dose, but overall clinical symptoms and survival were not significantly improved. However, GC-376 treatment led to milder tissue lesions, reduced viral loads, and decreased inflammation in mice challenged with a low virus dose.

SCIENTIFIC REPORTS (2021)

Review Chemistry, Multidisciplinary

Synthesis and Versatile Utilization of2-PyridylandPyrimidyl-RelatedReagents

Jae In Lee

BULLETIN OF THE KOREAN CHEMICAL SOCIETY (2020)

Article Chemistry, Organic

Acceptor-Controlled Transfer Dehydration of Amides to Nitriles

Hiroyuki Okabe et al.

ORGANIC LETTERS (2019)

Article Chemistry, Multidisciplinary

The E factor 25 years on: the rise of green chemistry and sustainability

Roger A. Sheldon

GREEN CHEMISTRY (2017)

Article Chemistry, Multidisciplinary

Pot economy and one-pot synthesis

Yujiro Hayashi

CHEMICAL SCIENCE (2016)

Article Chemistry, Multidisciplinary

A survey of solvent selection guides

Denis Prat et al.

GREEN CHEMISTRY (2014)

Article Chemistry, Multidisciplinary

The E factor: fifteen years on

Roger A. Sheldon

GREEN CHEMISTRY (2007)

Article Biochemistry & Molecular Biology

Methyl methanesulfonate (MMS) produces heat-labile DNA damage but no detectable in vivo DNA double-strand breaks

C Lundin et al.

NUCLEIC ACIDS RESEARCH (2005)