4.7 Article

Synthesis and structure-activity relationship studies of benzimidazole-thioquinoline derivatives as α-glucosidase inhibitors

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 Biochemistry & Molecular Biology

One-pot multi-component synthesis of novel chromeno[4,3-b]pyrrol-3-yl derivatives as alpha-glucosidase inhibitors

Malihe Karami et al.

Summary: A green and efficient one-pot multi-component protocol was developed to synthesize novel dihydrochromeno[4,3-b]pyrrol-3-yl derivatives that exhibited potent inhibitory activities against alpha-glucosidase. The most effective derivative showed a competitive mechanism with a Ki value of 42.6 μM, and docking studies revealed effective interaction with important residues in the active site of alpha-glucosidase.

MOLECULAR DIVERSITY (2022)

Article Chemistry, Physical

Synthesis and characterization of 1-amidino-O-alkylureas metal complexes as α- glucosidase Inhibitors: Structure-activity relationship, molecular docking, and kinetic studies

Firouz Matloubi Moghaddam et al.

Summary: This study synthesized and screened metal complexes as alpha-Glucosidase inhibitors, with Cu (II) complexes showing superior potency. The [Cu(L-Me)(2)](Cl)(2) complex exhibited the strongest inhibition against alpha-Glucosidase, comparable to acarbose. These findings were supported by molecular docking of ligands and enzyme interactions.

JOURNAL OF MOLECULAR STRUCTURE (2022)

Article Multidisciplinary Sciences

Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors

Aida Iraji et al.

Summary: A series of newly designed and synthesized cyanoacetohydrazide linked to 1,2,3-triazoles compounds were evaluated for their anti-alpha-glucosidase activity. Most of the synthesized compounds showed excellent inhibitory potential, with 9b and 9e exhibiting the highest activity. Kinetic binding studies and fluorescence measurements confirmed the interaction between these compounds and the enzyme.

SCIENTIFIC REPORTS (2022)

Article Chemistry, Multidisciplinary

New solid phase methodology for the synthesis of biscoumarin derivatives: experimental and in silico approaches

Elham Zarenezhad et al.

Summary: This study presents a simple and greener approach for the synthesis of biscoumarin derivatives using nano-MoO3 as a catalyst under mortar-pestle grinding. The synthesized derivatives showed good to excellent yields and were identified as alpha-glucosidase inhibitors. Computational investigations, including similarity searches and molecular docking studies, were performed to identify potential biological targets and determine detailed binding modes and critical interactions. The results suggest that the developed protocols offer an attractive pathway for the synthesis of biologically remarkable pharmacophores.

BMC CHEMISTRY (2022)

Article Chemistry, Multidisciplinary

Design, synthesis, and molecular docking studies of diphenylquinoxaline-6-carbohydrazide hybrids as potent α-glucosidase inhibitors

Keyvan Pedrood et al.

Summary: A novel series of diphenylquinoxaline-6-carbohydrazide hybrids were designed and synthesized as anti-diabetic agents. These compounds showed good inhibitory activity against alpha-glucosidase, with the most potent derivative 7e exhibiting competitive inhibition. Molecular docking studies revealed the binding mode of these derivatives within the active site of the enzyme, confirming the experimental results.

BMC CHEMISTRY (2022)

Article Chemistry, Physical

Design, synthesis, and in silico studies of benzimidazole bearing phenoxyacetamide derivatives as a-glucosidase and a-amylase inhibitors

Nahal Shayegan et al.

Summary: Benzimidazole bearing phenoxyacetamide derivatives 7a-l were designed and synthesized as anti-diabetic agents. The compounds exhibited varying degrees of α-glucosidase inhibitory activity, with the methoxy substituent on the phenoxy linker and the 4-F and 4-Cl substitutions at the Y position playing important roles in improving potency. The synthesized derivatives showed moderate to weak inhibitory activities against α-amylase, but specific compounds demonstrated strong inhibition.

JOURNAL OF MOLECULAR STRUCTURE (2022)

Review Chemistry, Multidisciplinary

A review on α-glucosidase inhibitory activity of first row transition metal complexes: a futuristic strategy for treatment of type 2 diabetes

Marzieh Sohrabi et al.

Summary: Type 2 diabetes mellitus is a global public health issue, and inhibition of alpha-glucosidase is the main therapeutic approach. Development of non-sugar based inhibitors is gaining attention in addition to research on sugar-based inhibitors. Metal complexes' in vitro anti-alpha-glucosidase activity is attracting increasing attention.

RSC ADVANCES (2022)

Article Biochemistry & Molecular Biology

Synthesis of 4-alkylaminoimidazo[1,2-a]pyridines linked to carbamate moiety as potent α-glucosidase inhibitors

Mina Saeedi et al.

Summary: A series of imidazo[1,2-a]pyridines linked to carbamate moiety were designed, synthesized, and evaluated for their alpha-glucosidase inhibitory activity. Compound 6d exhibited the most potent inhibition with a competitive mechanism, as supported by kinetic and molecular docking studies. Hydrogen bonds and electrostatic interactions in the active site contributed to the well-oriented conformation of compound 6d.

MOLECULAR DIVERSITY (2021)

Article Genetics & Heredity

Pharmacogenetic Testing of Cytochrome P450 Drug Metabolizing Enzymes in a Case Series of Patients with Prader-Willi Syndrome

Janice Forster et al.

Summary: In a clinical case series of 35 patients with Prader-Willi syndrome (PWS), pharmacogenetic testing revealed variations in CYP enzyme activity, particularly showing differences in metabolizing status for different genetic subtypes of PWS. This information may help inform dosage parameters and risk assessment for psychotropic medications in PWS patients.
Article Medicine, General & Internal

Medication adherence to injectable glucagon-like peptide-1 (GLP-1) receptor agonists dosed once weekly vs once daily in patients with type 2 diabetes: A meta-analysis

Erin R. Weeda et al.

Summary: This meta-analysis compared adherence to injectable GLP-1RAs dosed once weekly vs once daily in patients with type 2 diabetes (T2D), finding that once weekly dosing was associated with better adherence.

INTERNATIONAL JOURNAL OF CLINICAL PRACTICE (2021)

Article Multidisciplinary Sciences

Design, synthesis, biological evaluation, and molecular modeling studies of pyrazole-benzofuran hybrids as new α-glucosidase inhibitor

Fateme Azimi et al.

Summary: New derivatives of biphenyl pyrazole-benzofuran hybrids were synthesized and evaluated for their inhibitory effect against alpha-glucosidase activity in vitro. The most active compound 8e was identified as a competitive inhibitor of alpha-glucosidase. Molecular docking and dynamic simulations revealed the interaction modes of the compounds with the enzyme's active site.

SCIENTIFIC REPORTS (2021)

Article Biochemistry & Molecular Biology

Synthesis, in vitro evaluation, and molecular docking studies of novel hydrazineylideneindolinone linked to 1,2,3-triazole derivatives as potential α-glucosidase inhibitors

Diba Shareghi-Boroujeni et al.

Summary: A novel series of compounds were synthesized and evaluated for their anti-alpha-glucosidase activity, with compound 9d showing the best inhibitory activity with a 46-fold improvement compared to the positive control. Experimental results suggest these compounds as potential candidates for anti-diabetic agents.

BIOORGANIC CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Design and synthesis of novel quinazolinone-pyrazole derivatives as potential α-glucosidase inhibitors: Structure-activity relationship, molecular modeling and kinetic study

Fateme Azimi et al.

Summary: The study identified new compounds with enhanced alpha-glucosidase inhibitory activity, with variations in inhibitory activities due to different substitutions on the phenyl rings of diphenyl pyrazole moiety. The most potent compound inhibited the enzyme competitively with a Ki of 56 μM. Molecular docking analysis showed that key pharmacophoric moieties were crucial for binding interaction. Additionally, molecular dynamic investigations revealed structural perturbations and dynamic behaviors in the presence of the most active compound compared to the standard acarbose.

BIOORGANIC CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies

Muhammad Taha et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Review Chemistry, Medicinal

Synthetic heterocyclic candidates as promising α-glucosidase inhibitors: An overview

Manoj Dhameja et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Biochemistry & Molecular Biology

Flavonoids and Their Anti-Diabetic Effects: Cellular Mechanisms and Effects to Improve Blood Sugar Levels

Raghad Khalid AL-Ishaq et al.

BIOMOLECULES (2019)

Article Biochemistry & Molecular Biology

Biological evaluation of new imidazole derivatives tethered with indole moiety as potent α-glucosidase inhibitors

Sadia Naureen et al.

BIOORGANIC CHEMISTRY (2018)

Review Chemistry, Medicinal

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

Clementina M. M. Santos et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Editorial Material Medicine, General & Internal

Management of Type 2 Diabetes in 2017 Getting to Goal

Jane E. B. Reusch et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2017)

Article Chemistry, Medicinal

Synthesis of 2-phenyl-1H-imidazo[4,5-b]pyridine as type 2 diabetes inhibitors and molecular docking studies

Muhammad Taha et al.

MEDICINAL CHEMISTRY RESEARCH (2017)

Article Pharmacology & Pharmacy

Worldwide Distribution of Cytochrome P450 Alleles: A Meta-analysis of Population-scale Sequencing Projects

Y. Zhou et al.

CLINICAL PHARMACOLOGY & THERAPEUTICS (2017)

Article Biochemistry & Molecular Biology

Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies

Nik Khairunissa Nik Abdullah Zawawi et al.

BIOORGANIC CHEMISTRY (2016)

Article Biochemistry & Molecular Biology

Synthesis, α-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles

Muhammad Taha et al.

BIOORGANIC CHEMISTRY (2016)

Review Pharmacology & Pharmacy

Therapeutic potential of α-glucosidase inhibitors in type 2 diabetes mellitus: an evidence-based review

Shashank R. Joshi et al.

EXPERT OPINION ON PHARMACOTHERAPY (2015)

Article Chemistry, Medicinal

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

Douglas E. V. Pires et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Synthesis and molecular docking studies of potent α-glucosidase inhibitors based on biscoumarin skeleton

Khalid Mohammed Khan et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Biochemistry & Molecular Biology

α-Glucosidase inhibition by luteolin: Kinetics, interaction and molecular docking

Jiakai Yan et al.

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES (2014)

Article Food Science & Technology

Quinoline-2-carboxylic Acid Isolated from Ephedra pachyclada and Its Structural Derivatives Show Inhibitory Effects against α-Glucosidase and α-Amylase

Hwa-Won Lee et al.

JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Docking and SAR studies of salacinol derivatives as α-glucosidase inhibitors

Shinya Nakamura et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)