4.6 Article

New Hybrid Tetrahydropyrrolo[3,2,1-ij]quinolin-1-ylidene-2-thioxothiazolidin-4-ones as New Inhibitors of Factor Xa and Factor XIa: Design, Synthesis, and In Silico and Experimental Evaluation

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。
Review Medicine, Research & Experimental

Review of anticancer potentials and structure-activity relationships (SAR) of rhodanine derivatives

Lim Ju Yin et al.

Summary: Rhodanine is a privileged scaffold in medicinal chemistry with significant potential for cancer treatment, demonstrating broad biological activities and structural diversification for effective drug discovery. Rhodanine-derived compounds have shown promising anticancer activity while maintaining low cytotoxicity, highlighting their value for future cancer drug development.

BIOMEDICINE & PHARMACOTHERAPY (2022)

Article Chemistry, Medicinal

Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs

Xiaoan Li et al.

Summary: Thrombus is a major threat to human health, and the prevalence of cardio-cerebrovascular diseases caused by thrombus is increasing globally. Anticoagulant drugs are commonly used to treat thrombotic disorders, but current drugs have limitations. Therefore, there is a need to develop more effective antithrombotic drugs to tackle the challenges of thrombotic diseases.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

New Blood Coagulation Factor XIIa Inhibitors: Molecular Modeling, Synthesis, and Experimental Confirmation

Anna Tashchilova et al.

Summary: Complications caused by disorders in the blood coagulation system are prevalent in various medical fields, highlighting the need for the development of new and advanced drugs. This study utilized computational methods to search for potential low-molecular-weight noncovalent factor XIIa inhibitors, resulting in the identification of four compounds. Selectivity testing revealed that two of these inhibitors showed selectivity over other coagulation factors.

MOLECULES (2022)

Review Biochemistry & Molecular Biology

Anticancer Profile of Rhodanines: Structure-Activity Relationship (SAR) and Molecular Targets-A Review

Jacek Szczepanski et al.

Summary: Rhodanine is a well-known privileged heterocycle in medicinal chemistry with diverse biological activities, including anticancer properties. This review focuses on analyzing the anticancer features of rhodanines described in scientific literature over the past decade, discussing the structure-activity relationship of rhodanine derivatives and potential molecular targets.

MOLECULES (2022)

Review Chemistry, Medicinal

The Importance of Rhodanine Scaffold in Medicinal Chemistry: A Comprehensive Overview

Arif Mermer

Summary: Rhodanine-based compounds have shown broad biological activities through various modifications to the rhodanine ring, making them important in drug discovery.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

Coumarin-1,2,3-triazole Hybrid Molecules: An Emerging Scaffold for Combating Drug Resistance

Harish C. Upadhyay

Summary: The widespread use of antibiotics has led to bacterial resistance and recurrent infections. To overcome this issue, multidrug therapy or single drugs acting on multiple targets may be utilized. Natural product-based hybrid molecules may provide a super alternative to combat drug resistance caused by various bacterial and fungal strains.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

Pyrazole-based analogs as potential antibacterial agents against methicillin-resistance staphylococcus aureus (MRSA) and its SAR elucidation

Rameshwari Verma et al.

Summary: MRSA poses a deadly threat to humanity due to its easy transmission and resistance to antibiotics, including vancomycin. The development of new, efficient, and nontoxic drug candidate to fight against MRSA isolates is urgently needed. Research on pyrazole-containing derivatives has shown promise in combating MRSA with a broad antibacterial movement.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

Novel Hybrid Molecules Based on triazole-β-lactam as Potential Biological Agents

Pezhman Shiri

Summary: Triazole ring is a cyclic scaffold with three nitrogen heteroatoms that exhibit diverse biological activities. The hybrid approach is an innovative tool for synthesizing multiple entities in one molecule with novel biological properties. Various synthetic protocols exist for beta-lactam synthesis, with the Staudinger reaction being a successful strategy.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

Antitubercular properties of thiazolidin-4-ones - A review

Nazar Trotsko

Summary: The thiazolidin-4-one scaffold is widely used in medicinal chemistry due to its broad biological activity, particularly in the field of anti-tuberculosis activity. Some compounds derived from this scaffold have shown promising anti-tuberculosis activity, outperforming reference drugs against various strains of Mycobacterium tuberculosis. The structure-activity relationship (SAR) and potential molecular targets of these compounds were also discussed in the review.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

α-Glucosidase, α-Amylase Inhibition, Kinetics and Docking Studies of Novel (2-Chloro-6-(trifluoromethyl)benzyloxy)arylidene) Based Rhodanine and Rhodanine Acetic Acid Derivatives

Vasantha Kumar et al.

Summary: In the study, a novel series of fluorinated compounds were synthesized and screened for their potential as antidiabetic agents, with two compounds identified as promising alpha-glucosidase inhibitors. Further kinetic inhibition experiments confirmed their competitive inhibitory nature. Molecular docking studies on alpha-glucosidase indicated the key role of substituent position in inhibitory potential.

CHEMISTRYSELECT (2021)

Review Pharmacology & Pharmacy

Drug screening of rhodanine derivatives for antibacterial activity

Suresh Maddila et al.

EXPERT OPINION ON DRUG DISCOVERY (2020)

Review Chemistry, Medicinal

Hybrid molecules based on 1,3,5-triazine as potential therapeutics: A focused review

Parteek Prasher et al.

DRUG DEVELOPMENT RESEARCH (2020)

Review Chemistry, Multidisciplinary

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Pravati Panda et al.

CHEMISTRYSELECT (2020)

Review Chemistry, Multidisciplinary

Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids

Prashant S. Auti et al.

RSC ADVANCES (2020)

Review Biotechnology & Applied Microbiology

A conceptual review of rhodanine: current applications of antiviral drugs, anticancer and antimicrobial activities

Seyyed Mojtaba Mousavi et al.

ARTIFICIAL CELLS NANOMEDICINE AND BIOTECHNOLOGY (2019)

Review Chemistry, Medicinal

Molecular Hybridization as a Tool for Designing Multitarget Drug Candidates for Complex Diseases

Viktoriya Ivasiv et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2019)

Article Biochemical Research Methods

New factor Xa inhibitors based on 1,2,3,4-tetrahydroquinoline developed by molecular modelling

Ivan Ilin et al.

JOURNAL OF MOLECULAR GRAPHICS & MODELLING (2019)

Review Chemistry, Medicinal

Hybrid Molecules Development: A Versatile Landscape for the Control of Aritifungal Drug Resistance: A Review

Chioma G. Anusionwu et al.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors

Zilun Hu et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2018)

Article Chemistry, Medicinal

Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors

Hong Jiang et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2018)

Article Chemistry, Medicinal

Factor XIa Inhibitors as New Anticoagulants

Mimi L. Quan et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Multidisciplinary

Hybrid organic molecules as antiinflammatory agents; a review of structural features and biological activity

Noor ul Amin Mohsin et al.

TURKISH JOURNAL OF CHEMISTRY (2018)

Review Pharmacology & Pharmacy

Recent developments with rhodanine as a scaffold for drug discovery

Danylo Kaminskyy et al.

EXPERT OPINION ON DRUG DISCOVERY (2017)

Article Chemistry, Medicinal

Discovery of a Parenteral Small Molecule Coagulation Factor Xla Inhibitor Clinical Candidate (BMS-962212)

Donald J. P. Pinto et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Mathematics, Applied

INFLUENCE OF THE METHOD OF HYDROGEN ATOMS INCORPORATION INTO THE TARGET PROTEIN ON THE PROTEIN-LIGAND BINDING ENERGY

D. C. Kutov et al.

BULLETIN OF THE SOUTH URAL STATE UNIVERSITY SERIES-MATHEMATICAL MODELLING PROGRAMMING & COMPUTER SOFTWARE (2017)

Article Biochemistry & Molecular Biology

Effects of 8-halo-7-deaza-2′-deoxyguanosine triphosphate on DNA synthesis by DNA polymerases and cell proliferation

Yizhen Yin et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2016)

Article Biochemistry & Molecular Biology

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

James R. Corte et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation

Dnyaneshwar D. Subhedar et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

Review Chemistry, Medicinal

Hybrid molecules: The privileged scaffolds for various pharmaceuticals

Shaveta et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Biochemistry & Molecular Biology

From hybrid compounds to targeted drug delivery in antimalarial therapy

Rudi Oliveira et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Pyridine and pyridinone-based factor XIa inhibitors

James R. Corte et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Article Chemistry, Medicinal

Design, synthesis and structural exploration of novel fluorinated dabigatran derivatives as direct thrombin inhibitors

Mei-Lin Li et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Cardiac & Cardiovascular Systems

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

Pancras C. Wong et al.

JOURNAL OF THROMBOSIS AND THROMBOLYSIS (2015)

Article Biotechnology & Applied Microbiology

Application of Molecular Modeling to Development of New Factor Xa Inhibitors

Vladimir B. Sulimov et al.

BIOMED RESEARCH INTERNATIONAL (2015)

Article Chemistry, Organic

New Heterocyclic Systems Based on Substituted 3,4-Dihydro-1H-Spiro[Quinoline-2,1'-Cycloalkanes]

S. M. Medvedeva et al.

CHEMISTRY OF HETEROCYCLIC COMPOUNDS (2014)

Article Chemistry, Medicinal

Halogen-enriched fragment libraries as chemical probes for harnessing halogen bonding in fragment-based lead discovery

Markus O. Zimmermann et al.

FUTURE MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

Mimi L. Quan et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Editorial Material Multidisciplinary Sciences

Chemical con artists foil drug discovery

Jonathan Baell et al.

NATURE (2014)

Article Chemistry, Medicinal

Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents

Meng Guo et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)

Article Chemistry, Medicinal

Application of the Docking Program SOL for CSAR Benchmark

Alexey V. Sulimov et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2013)

Article Chemistry, Multidisciplinary

Avogadro: an advanced semantic chemical editor, visualization, and analysis platform

Marcus D. Hanwell et al.

JOURNAL OF CHEMINFORMATICS (2012)

Article Chemistry, Medicinal

Observations on screening-based research and some concerning trends in the literature

Jonathan B. Baell

FUTURE MEDICINAL CHEMISTRY (2010)

Review Biochemistry & Molecular Biology

Rhodanine as a Privileged Scaffold in Drug Discovery

T. Tomasic et al.

CURRENT MEDICINAL CHEMISTRY (2009)

Article Chemistry, Medicinal

Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with biaryl P4 motifs

Robert J. Young et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Review Chemistry, Medicinal

Recent advances in the development of hybrid molecules/designed multiple compounds with antiamnesic properties

Michael Decker

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2007)