Discovery of Thiazole Carboxamides as Novel Vanin-1 Inhibitors for Inflammatory Bowel Disease Treatment DOI
Tao Xie, G. F. Cao,

Shize Zhang

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(22), P. 20372 - 20398

Published: Nov. 8, 2024

Inflammatory bowel disease (IBD) is a clinically heterogeneous demanding more therapeutic targets and intervention strategies. Vanin-1, an oxidative stress-regulating protein, has emerged as promising target for alleviating inflammation stress. In this study, series of thiazole carboxamide derivatives vanin-1 inhibitors were designed synthesized. The preferred compound,

Language: Английский

Recent Advances in SARS-CoV-2 Main Protease Inhibitors: From Nirmatrelvir to Future Perspectives DOI Creative Commons
Andrea Citarella, Alessandro Dimasi, Davide Moi

et al.

Biomolecules, Journal Year: 2023, Volume and Issue: 13(9), P. 1339 - 1339

Published: Sept. 2, 2023

The main protease (Mpro) plays a pivotal role in the replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and is considered highly conserved viral target. Disruption catalytic activity Mpro produces detrimental effect on course infection, making this target one most attractive for treatment COVID-19. current success SARS-CoV-2 inhibitor Nirmatrelvir, first oral drug forms COVID-19, has further focused attention researchers important target, search new inhibitors thriving exciting field development antiviral drugs active against related coronaviruses.

Language: Английский

Citations

29
The expanding repertoire of covalent warheads for drug discovery DOI
Namrashee V. Mehta, Mariam S. Degani

Drug Discovery Today, Journal Year: 2023, Volume and Issue: 28(12), P. 103799 - 103799

Published: Oct. 13, 2023

Language: Английский

Citations

24
On the origins of SARS-CoV-2 main protease inhibitors DOI
Yves L. Janin

RSC Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 15(1), P. 81 - 118

Published: Oct. 13, 2023

In order to address the world-wide health challenge caused by COVID-19 pandemic, 3CL protease/SARS-CoV-2 main protease (SARS-CoV-2-M

Language: Английский

Citations

19
Non-peptidic inhibitors targeting SARS-CoV-2 main protease: A review DOI

Ya-Qi Xiao,

Jiao Long, Shuang‐Shuang Zhang

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 147, P. 107380 - 107380

Published: April 16, 2024

Language: Английский

Citations

9
Progress in Research on Inhibitors Targeting SARS-CoV-2 Main Protease (Mpro) DOI Creative Commons
Yue Yang,

Yidan Luo,

Chenbo Zhang

et al.

ACS Omega, Journal Year: 2024, Volume and Issue: 9(32), P. 34196 - 34219

Published: Aug. 2, 2024

Since 2019, the novel coronavirus (SARS-CoV-2) has caused significant morbidity and millions of deaths worldwide. The Coronavirus Disease 2019 (COVID-19), by SARS-CoV-2 its variants, further highlighted urgent need for development effective therapeutic agents. Currently, highly conserved broad-spectrum nature main proteases (M

Language: Английский

Citations

6
Design, synthesis and activity evaluation of 4-(quinoline-2-yl)aniline derivatives as SARS-CoV‑2 main protease inhibitors DOI

Honglei Bao,

Hui Meng, Shilin Gong

et al.

Bioorganic & Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 121, P. 118135 - 118135

Published: Feb. 26, 2025

Language: Английский

Citations

0
Recent breakthroughs in synthetic small molecules targeting SARS-CoV-2 Mpro from 2022 to 2024 DOI
Laura Braconi, Alice Sosic, Letizia Crocetti

et al.

Bioorganic & Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 128, P. 118247 - 118247

Published: May 20, 2025

Language: Английский

Citations

0
N-Acylbenzimidazoles as Selective Acylators of the Catalytic Cystein of the Coronavirus 3CL Protease. DOI

Fatima-Zahra Chaibi,

Lucile Brier, Paul Carré

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 276, P. 116707 - 116707

Published: July 24, 2024

Language: Английский

Citations

3
Crystallographic Data Collection Using a Multilayer Monochromator on an Undulator Beamline at the Shanghai Synchrotron Radiation Facility DOI Creative Commons
Chenyu Zhang,

Xu Qin,

Weiwei Wang

et al.

Crystals, Journal Year: 2024, Volume and Issue: 14(2), P. 199 - 199

Published: Feb. 19, 2024

To resolve photons hungry for weak diffraction samples by the crystallographic method, a double-multilayer monochromator (DMM) was employed on an undulator beamline (BL17UM) at Shanghai Synchrotron Radiation Facility (SSRF) to provide focused sub-micron beam with high brightness macromolecular crystallography experiments. High-quality datasets from model protein crystal were collected and processed existing program structure solution refinement. The data quality compared normal silicon evaluate bandwidth of DMM effect these data. This experiment demonstrates that multilayer optics may play valuable role in satisfying demands structure-related research, which requires novel methods.

Language: Английский

Citations

1
Highly Selective C–N and C–S Dual Functionalization of 1,3-Dicarbonyl Derivatives Using TBHP as an Oxidant DOI

Pooja K. Bagad,

Ratanamala S. Darole, Gamidi Rama Krishna

et al.

The Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 89(13), P. 9371 - 9380

Published: June 24, 2024

A direct electrosynthesis/photocatalyst-free, atom-economical, and efficient method for the selective synthesis of (E)-3-amino-2-thiocyanato-α,β-unsaturated carbonyl compounds is described through a given protocol. The present approach features use inexpensive ammonium thiocyanate to achieve dual functionalization 1,3-dicarbonyl using TBHP as an oxidant, providing rapid practical route formation both C–N C–S bonds via radical process. This offers broad substrate scope with excellent yield allows further exploration products construct heterocyclic other functionalities.

Language: Английский

Citations

1