Molybdenum‐Promoted Synthesis of Benzo[4,5]imidazo[1,2‐c]quinazolin‐6(5H)‐ones via Nitro Reduction and Ring Expansion DOI
Ran Zhao,

Zerui Meng,

Xiaoru Meng

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(34)

Published: Sept. 9, 2024

Abstract A simple and efficient method to construct benzo[4,5]imidazo[1,2‐ c ]quinazolin‐6(5 H )‐one skeleton was reported. powerful functional group transformation strategy of −NO 2 transformed into −NH involved in this method. Only Mo(CO) 6 used the reaction, which acted as both reductant cyclization accelerator. And a series derivatives were obtained.

Language: Английский

Rational Molecular Editing: A New Paradigm in Drug Discovery DOI Creative Commons
Chunhua Ma, Craig W. Lindsley, Junbiao Chang

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(14), P. 11459 - 11466

Published: June 21, 2024

ADVERTISEMENT RETURN TO ARTICLES ASAPPREVEditorialNEXTRational Molecular Editing: A New Paradigm in Drug DiscoveryChunhua MaChunhua MaState Key Laboratory of Antiviral Drugs, Pingyuan Laboratory, NMPA for Research and Evaluation Innovative Drug, School Chemistry Chemical Engineering, Henan Normal University, Xinxiang, 453007, ChinaMore by Chunhua Mahttps://orcid.org/0000-0001-7613-6471, Craig W. Lindsley*Craig LindsleyVanderbilt University Medical Center, Franklin, Tennessee 37027, United States*E-mail: [email protected]More Lindsleyhttps://orcid.org/0000-0003-0168-1445, Junbiao Chang*Junbiao ChangCollege Chemistry, State Zhengzhou 450001, China*E-mail: Chang, Bin Yu*Bin YuCollege Yuhttps://orcid.org/0000-0002-7207-643XCite this: J. Med. Chem. 2024, XXXX, XXX, XXX-XXXPublication Date (Web):June 21, 2024Publication History Received13 June 2024Published online21 2024https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c01347https://doi.org/10.1021/acs.jmedchem.4c01347editorialACS PublicationsPublished 2024 American Society. This publication is available under these Terms Use. Request reuse permissions free to access through this site. Learn MoreArticle Views-Altmetric-Citations-LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum full text article downloads since November 2008 (both PDF HTML) across all institutions individuals. These metrics regularly updated reflect usage leading up last few days.Citations number other articles citing article, calculated Crossref daily. Find more information about citation counts.The Altmetric Attention Score a quantitative measure attention that research has received online. Clicking on donut icon will load page at altmetric.com with additional details score social media presence given article. how calculated. Share Add toView InAdd Full Text ReferenceAdd Description ExportRISCitationCitation abstractCitation referencesMore Options onFacebookTwitterWechatLinked InRedditEmail (2 MB) Get e-AlertscloseSUBJECTS:Drug discovery,Macrocyclization,Molecules,Pharmaceuticals,Scaffolds e-Alerts

Language: Английский

Citations

20
Recent progress in visible light‐driven halogenation: Chlorination, bromination, and iodination DOI

Anh Thu Nguyen,

Houng Kang, Truong Giang Luu

et al.

Bulletin of the Korean Chemical Society, Journal Year: 2024, Volume and Issue: 45(9), P. 738 - 758

Published: Sept. 1, 2024

Abstract Halogenation is one of the most important transformations in organic synthesis. Halogenated compounds are employed many reactions to prepare useful molecules. Many methods have been developed introduce halogens into different compounds. Visible light‐mediated efficient, low‐toxic, and mild‐condition applied for various chemistry transformations. Remarkably, there has an increasing development application visible light‐induced halogenation recent years. Herein, we present a comprehensive summary including chlorination, bromination, iodination under light irradiation since 2020.

Language: Английский

Citations

5
Pyridazine: A privileged scaffold in the development of 21st-century pesticides DOI
Chao Chen, Geng Wang, Ke Li

et al.

Chinese Chemical Letters, Journal Year: 2025, Volume and Issue: unknown, P. 110902 - 110902

Published: Jan. 1, 2025

Language: Английский

Citations

0
Synthetic Approaches to the New Drugs Approved during 2023 DOI
Scott P. France,

Erick A. Lindsey,

Emma L. McInturff

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 3, 2025

This review is the next installment of an annual series that discusses synthetic routes to access 28 small molecule drugs were approved worldwide in 2023. A brief description each drug's mechanism action, history its discovery and development, approaches published primary or patent literature most likely used for clinical studies development are included. Synthetic chemistry, convert complex intermediates active compounds build a new drug from basic building block chemicals, critical delivery treatments disease patients.

Language: Английский

Citations

0
Identification of 6,9-dihydro-5H-pyrrolo[3,2-h]quinazolines as a new class of F508del-CFTR correctors for the treatment of cystic fibrosis DOI Creative Commons
Marilia Barreca,

Mario Renda,

Virginia Spanò

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 276, P. 116691 - 116691

Published: July 20, 2024

Although substantial advances have been obtained in the pharmacological treatment of cystic fibrosis (CF) with approval Kaftrio, a combination two correctors (VX-661, VX-445) and one potentiator (VX-770), new modulators are still needed to rescue F508del other CFTR mutants trafficking defects. We previously identified PP compounds based on tricyclic core as high efficacy F508del-CFTR native epithelial cells CF patients, particularly class 1 (VX-809, VX-661). Compound PP028 was found lead candidate for used mechanistic insight indicating that behaves 3 corrector, similarly VX-445. From exploration chemical space around hit structure, iterative cycles synthesis functional testing, 6,9-dihydro-5H-pyrrolo [3,2-h]quinazolines corrector activity discovered. Within series 38 analogues, derivatives emerged promising candidates further assess mechanism action. Both compounds, decorated benzensulfonylamino group at pyrimidine moiety, were able generate dose-dependent increase function, presence VX-809. Half-effective concentrations (EC

Language: Английский

Citations

2
Visible-Light-Mediated Azidation of α-Diazoesters with TMSN3 via Direct Photoexcitation and SH2 Mechanism DOI
Jingya Yang, Sheng-Yu Wang,

Yating Han

et al.

The Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 89(16), P. 11707 - 11715

Published: July 30, 2024

A visible light-mediated azidation of α-diazoesters with TMSN

Language: Английский

Citations

1
The therapeutic effect of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol on chemically induced atopic dermatitis DOI Creative Commons

Su‐Hyun Shin,

Yu Jin Kim, Su Jin Kim

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Oct. 8, 2024

Atopic dermatitis (AD) is the most common chronic inflammatory skin disease worldwide. However, it still urgent to develop innovative treatments that can effectively manage refractory patients with unpredictable courses. In this study, we evaluated therapeutic efficacy of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) as a novel agent for AD treatment using human-like mouse model AD. PLAG significantly improved 2,4-dinitrochlorobenzene (DNCB)-induced lesions compared those in mice treated DNCB alone. substantially modulated AD-induced infiltration monocytes and eosinophils into humoral systemic responses involving immunoglobulin E (IgE), interleukin (IL)-4, IL-13, restoring them normal state. Next, abrocitinib severe treatment. exhibited significant effect on abrocitinib. Unlike abrocitinib, reduced eosinophil level similar observed untreated negative controls. Notably, both downregulated IgE, IL-4, IL-13 pattern, reaching levels Our findings strongly suggest may serve an comparable

Language: Английский

Citations

1
The therapeutic effect of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol on chemically induced atopic dermatitis DOI Creative Commons

Su‐Hyun Shin,

Yu Jin Kim, Su Jin Kim

et al.

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: May 15, 2024

Abstract Atopic dermatitis (AD) is the most common chronic inflammatory skin disease worldwide. However, it still urgent to develop innovative treatments that can effectively manage refractory patients with unpredictable courses. In this study, we evaluated therapeutic efficacy of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) as a novel agent for AD treatment using human-like mouse model AD. PLAG significantly improved 2,4-dinitrochlorobenzene (DNCB)-induced lesions compared those in mice treated DNCB alone. substantially modulated AD-induced infiltration monocytes and eosinophils into humoral systemic responses involving immunoglobulin E (IgE), interleukin (IL)-4, IL-13, restoring them normal state. Next, abrocitinib severe treatment. exhibited significant effect on abrocitinib. Unlike abrocitinib, reduced eosinophil level similar observed untreated negative controls. Notably, both downregulated IgE, IL-4, IL-13 pattern, reaching levels Our findings strongly suggest may serve an comparable

Language: Английский

Citations

0
Molybdenum‐Promoted Synthesis of Benzo[4,5]imidazo[1,2‐c]quinazolin‐6(5H)‐ones via Nitro Reduction and Ring Expansion DOI
Ran Zhao,

Zerui Meng,

Xiaoru Meng

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(34)

Published: Sept. 9, 2024

Abstract A simple and efficient method to construct benzo[4,5]imidazo[1,2‐ c ]quinazolin‐6(5 H )‐one skeleton was reported. powerful functional group transformation strategy of −NO 2 transformed into −NH involved in this method. Only Mo(CO) 6 used the reaction, which acted as both reductant cyclization accelerator. And a series derivatives were obtained.

Language: Английский

Citations

0