Synthesis, evaluation, and mechanism of 1-(4-(arylethylenylcarbonyl)phenyl)-4-carboxy-2-pyrrolidinones as potent reversible SARS-CoV-2 entry inhibitors

SARS‐CoV‐2 3CL pro displays faster self‐maturation in vitro than SARS‐CoV 3CL pro due to faster C‐terminal cleavage

(2022) Chih‐Jung Kuo et al.   FEBS LETTERS

Identification of Entry Inhibitors against Delta and Omicron Variants of SARS-CoV-2

(2022) Richard Kuan-Lin Lee et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic

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BA.2.12.1, BA.4 and BA.5 escape antibodies elicited by Omicron infection

(2022) Yunlong Cao et al.   NATURE

Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation

(2022) Bryan J. Fraser et al.   Nature Chemical Biology

Dual Inhibitors of Main Protease (MPro) and Cathepsin L as Potent Antivirals against SARS-CoV2

(2022) Santanu Mondal et al.   Journal of the American Chemical Society

Kinetic characterization and inhibitor screening for the proteases leading to identification of drugs against SARS-CoV-2

(2021) Chih-Jung Kuo et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication

(2021) Shin-ichiro Hattori et al.   Nature Communications

Small-Molecule Inhibitors of the Coronavirus Spike: ACE2 Protein–Protein Interaction as Blockers of Viral Attachment and Entry for SARS-CoV-2

(2021) Damir Bojadzic et al.   ACS Infectious Diseases

Identification of non-covalent 3C-like protease inhibitors against severe acute respiratory syndrome coronavirus-2 via virtual screening of a Korean compound library

(2021) Joo-Youn Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In vitro inhibition and molecular docking of a new ciprofloxacin‐chalcone against SARS‐CoV‐2 main protease

(2021) Rania Alaaeldin et al.   FUNDAMENTAL & CLINICAL PHARMACOLOGY

New Chalcone Derivatives as Effective Anti‐SARS‐CoV‐2 Agents

(2021) Nizami Duran et al.   INTERNATIONAL JOURNAL OF CLINICAL PRACTICE

Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure–Activity Relationship, and X-ray Structural Studies

(2021) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Perilla (Perilla frutescens) leaf extract inhibits SARS-CoV-2 via direct virus inactivation

(2021) Wen-Fang Tang et al.   Biomedical Journal

Chalcone Derivatives: Role in Anticancer Therapy

(2021) Yang Ouyang et al.   Biomolecules

Mechanisms of SARS-CoV-2 entry into cells

(2021) Cody B. Jackson et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells

(2021) Matthew Mahoney et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro

(2020) Manli Wang et al.   CELL RESEARCH

Genomic characterisation and epidemiology of 2019 novel coronavirus: implications for virus origins and receptor binding

(2020) Roujian Lu et al.   LANCET

Clinical features of patients infected with 2019 novel coronavirus in Wuhan, China

(2020) Chaolin Huang et al.   LANCET

A new coronavirus associated with human respiratory disease in China

(2020) Fan Wu et al.   NATURE

A pneumonia outbreak associated with a new coronavirus of probable bat origin

(2020) Peng Zhou et al.   NATURE

A Novel Coronavirus from Patients with Pneumonia in China, 2019

(2020) Na Zhu et al.   NEW ENGLAND JOURNAL OF MEDICINE

Nafamostat Mesylate Blocks Activation of SARS-CoV-2: New Treatment Option for COVID-19

(2020) Markus Hoffmann et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor

(2020) Markus Hoffmann et al.   CELL

Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potency

(2020) Calvin J. Gordon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pathogenesis and transmission of SARS-CoV-2 in golden hamsters

(2020) Sin Fun Sia et al.   NATURE

Structure of the SARS-CoV-2 spike receptor-binding domain bound to the ACE2 receptor

(2020) Jun Lan et al.   NATURE

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

(2020) Zhenming Jin et al.   NATURE

Compassionate Use of Remdesivir for Patients with Severe Covid-19

(2020) Jonathan Grein et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2020) Wenhao Dai et al.   SCIENCE

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

(2020) Linlin Zhang et al.   SCIENCE

An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice

(2020) Timothy P. Sheahan et al.   Science Translational Medicine

Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis

(2020) Deepthi Ramesh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Syrian hamsters as a small animal model for SARS-CoV-2 infection and countermeasure development

(2020) Masaki Imai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Anticoagulant Nafamostat Potently Inhibits SARS-CoV-2 S Protein-Mediated Fusion in a Cell Fusion Assay System and Viral Infection In Vitro in a Cell-Type-Dependent Manner

(2020) Mizuki Yamamoto et al.   Viruses-Basel

TMPRSS2 and furin are both essential for proteolytic activation of SARS-CoV-2 in human airway cells

(2020) Dorothea Bestle et al.   Life Science Alliance

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

(2020) Robert L. Hoffman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

(2020) Wayne Vuong et al.   Nature Communications

Furin Inhibitors Block SARS-CoV-2 Spike Protein Cleavage to Suppress Virus Production and Cytopathic Effects

(2020) Ya-Wen Cheng et al.   Cell Reports

Chalcone derivatives and their antibacterial activities: Current development

(2019) Man Xu et al.   BIOORGANIC CHEMISTRY

Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo

(2016) Jun Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

SARS and MERS: recent insights into emerging coronaviruses

(2016) Emmie de Wit et al.   NATURE REVIEWS MICROBIOLOGY

Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents

(2015) Ahmet Özdemir et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

pkCSM: Predicting Small-Molecule Pharmacokinetic and Toxicity Properties Using Graph-Based Signatures

(2015) Douglas E. V. Pires et al.   JOURNAL OF MEDICINAL CHEMISTRY

Copper/N,N-Dimethylglycine Catalyzed Goldberg Reactions Between Aryl Bromides and Amides, Aryl Iodides and Secondary Acyclic Amides

(2014) Liqin Jiang   MOLECULES

Sanjeevini: a freely accessible web-server for target directed lead molecule discovery

(2012) B Jayaram et al.   BMC BIOINFORMATICS

Open Babel: An open chemical toolbox

(2011) Noel M O'Boyle et al.   Journal of Cheminformatics