☆ 4.5 Article

Pyrazolidinone-based peptidomimetic SARS-CoV-2 Mpro inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2023)

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 Chemistry, Medicinal

Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability

Bing Bai et al.

Summary: This study describes novel antiviral compounds against coronaviruses, which have good activity and stability, and show effective inhibition of SARS-CoV-2 replication. They also exhibit better selectivity index and broad-spectrum antiviral activity against different types of coronaviruses.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine

Tika R. Malla et al.

Summary: This study describes the synthesis of penicillin derivatives and investigates their mechanism of inhibition on the SARS-CoV-2 main protease (M-pro) through mass spectrometric and crystallographic analyses. The results suggest that beta-lactams have potential as M-pro inhibitors by forming a stable acyl-enzyme complex through their reaction with the nucleophilic cysteine.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir

Subramanyam Vankadara et al.

Summary: The SARS-CoV-2 pandemic is causing an unprecedented global health emergency. The FDA has granted emergency use authorization to nirmatrelvir for treating infected patients. The study investigated nirmatrelvir analogs with different warheads and their inhibitory activities, finding that hydroxymethylketone and ketobenzothiazole warheads were equipotent to the nitrile warhead, suggesting their potential use for treating coronavirus infections.

ACS MEDICINAL CHEMISTRY LETTERS (2022)

添加到收藏夹

Review Medicine, Research & Experimental

The SARS-CoV-2 main protease (Mpro): Structure, function, and emerging therapies for COVID-19

Qing Hu et al.

Summary: This review focuses on the structural features and biological function of SARS-CoV-2 main protease (3CLpro) and the recent advances in developing 3CLpro inhibitors. The review comprehensively summarizes the characteristics of various 3CLpro inhibitors, highlights the challenges in this field, and proposes future research directions.

MEDCOMM (2022)

添加到收藏夹

Article Medicine, General & Internal

Safety and efficacy of the ChAdOx1 nCoV-19 vaccine (AZD1222) against SARS-CoV-2: an interim analysis of four randomised controlled trials in Brazil, South Africa, and the UK

Merryn Voysey et al.

Summary: The ChAdOx1 nCoV-19 vaccine has been shown to have an acceptable safety profile and effectiveness against symptomatic COVID-19, with higher efficacy observed in the group that received a low dose followed by a standard dose.

LANCET (2021)

添加到收藏夹

Article Chemistry, Multidisciplinary

Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors

Julian Breidenbach et al.

Summary: Two classes of protease inhibitors, azanitriles and pyridyl esters, were identified and optimized for potential use against COVID-19. Tailored peptides with unique azanitrile warheads showed promising results in inhibiting M-pro and cathepsin L. Through a focused approach, two irreversible inhibitors, azanitrile 8 and pyridyl ester 17, have been discovered as potential drug candidates for further development.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Lead compounds for the development of SARS-CoV-2 3CL protease inhibitors

Sho Iketani et al.

Summary: The study identifies three structurally diverse compounds as inhibitors of the SARS-CoV-2 3CL protease and provides insights for designing improved inhibitors.

NATURE COMMUNICATIONS (2021)

添加到收藏夹

Article Chemistry, Multidisciplinary

Mass spectrometry reveals potential of β-lactams as SARS-CoV-2 Mpro inhibitors

Tika R. Malla et al.

Summary: The study presents a high-throughput M-pro assay and identifies beta-lactams, including penicillin esters, as potential inhibitors of M-pro. These findings suggest the potential of acylating agents for M-pro inhibition in anti-viral chemotherapy.

CHEMICAL COMMUNICATIONS (2021)

添加到收藏夹

Article Chemistry, Medicinal

α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment

Linlin Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

Wenhao Dai et al.

SCIENCE (2020)

添加到收藏夹

Article Chemistry, Medicinal

A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli

Joel A. Goldberg et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

Zhenming Jin et al.

NATURE (2020)

添加到收藏夹

Review Chemistry, Medicinal

The development of Coronavirus 3C-Like protease (3CLpro) inhibitors from 2010 to 2020

Yuzhi Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19

Robert L. Hoffman et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Review Microbiology

Progress in Developing Inhibitors of SARS-CoV-2 3C-Like Protease

Qingxin Li et al.

MICROORGANISMS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?

Lorenzo Cianni et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

Matthias Gehringer et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Review Microbiology

Origin and evolution of pathogenic coronaviruses

Jie Cui et al.

NATURE REVIEWS MICROBIOLOGY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Non-classical transpeptidases yield insight into new antibacterials

Pankaj Kumar et al.

NATURE CHEMICAL BIOLOGY (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structural insight into the inactivation of Mycobacterium tuberculosis non-classical transpeptidase LdtMt2 by biapenem and tebipenem

Mario A. Bianchet et al.

BMC BIOCHEMISTRY (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

Thiol Probes To Detect Electrophilic Natural Products Based on Their Mechanism of Action

Gabriel Castro-Falcon et al.

ACS CHEMICAL BIOLOGY (2016)

添加到收藏夹

Article Chemistry, Medicinal

An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy

Thanigaimalai Pillaiyar et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Review Pharmacology & Pharmacy

Carbonyl reduction pathways in drug metabolism

Petra Malatkova et al.

DRUG METABOLISM REVIEWS (2014)

添加到收藏夹

Letter Cell Biology

Crystal structure of L,D-transpeptidase Ldt(Mt2) in complex with meropenem reveals the mechanism of carbapenem against Mycobacterium tuberculosis

Wen-Juan Li et al.

CELL RESEARCH (2013)

添加到收藏夹

Article Chemistry, Organic

A Convenient and Efficient Synthesis of Dipeptidyl Benzoxaboroles and Their Peptidomimetics

Zhengyan Fu et al.

SYNTHESIS-STUTTGART (2013)

添加到收藏夹

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of New Cinnamic Derivatives as Antituberculosis Agents

Prithwiraj De et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

添加到收藏夹

Article Chemistry, Multidisciplinary

Software News and Update AutoDock Vina: Improving the Speed and Accuracy of Docking with a New Scoring Function, Efficient Optimization, and Multithreading

Oleg Trott et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2010)

添加到收藏夹

Review Chemistry, Multidisciplinary

Irreversible inhibitors of serine, cysteine, and threonine proteases

JC Powers et al.

CHEMICAL REVIEWS (2002)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.