Synthesis and In-Vitro Antimycobacterial Evaluation of 4-Arylidene-2-Phenyl-6-(Aryl)-4,5-Dihydropyridazin-3(2H)-One Derivatives

Almehmadi, Mazen; Alsaiari, Ahad Amer; Asif, Mohammad

doi:10.1007/s11094-023-02876-3

Pharm Chem J

2023

DOI: 10.1007/s11094-023-02876-3

|View full text |Cite

Synthesis and In-Vitro Antimycobacterial Evaluation of 4-Arylidene-2-Phenyl-6-(Aryl)-4,5-Dihydropyridazin-3(2H)-One Derivatives

Mazen Almehmadi

Ahad Amer Alsaiari

Mohammad Asif

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2024

Publication Types

Select...

Article1

Relationship

Self Cite0

Independent1

Authors

Journals

Cited by 1 publication

References 43 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Pyridazine Derivatives as New Antidiabetic Agents: Synthesis, In‐Vitro α‐Amylase Inhibitory Activity, Molecular Docking and Molecular Dynamics Simulations Studies

Boukharsa,

Alhaji Isa,

Sayah

et al. 2024

ChemistrySelect

View full text Add to dashboard Cite

This study involved the synthesis, characterization, and assessment of fourteen pyridazine analogs (designated as 1–14) to investigate their efficacy in inhibiting the α‐amylase enzyme for potential diabetes treatment using an in vitro approach. Additionally, in silico molecular docking and molecular dynamic (MD) simulations were conducted to assess the inhibitory properties of these analogs. Physicochemical and pharmacokinetic properties of the fourteen pyridazine analogs were predicted using the DataWarrior tool. Results indicated that all tested compounds demonstrated significant α‐amylase inhibitory activity, with IC50 values ranging from 81.28±0.00 to 1623.54±2.67 μM compared to the standard drug acarbose (IC50=220.42±36.40 μM). Notably, compounds 8 and 12 exhibited the most potent α‐amylase inhibitory activity, with IC50 values of 81.28±0.00 μM and 200.60±34.65 μM, respectively. Molecular docking analysis revealed binding energies ranging from −7.53 to −5.77 kcal/mol and inhibition constants ranging from 3.00 to 58.96 μM, with compounds 9, 7, 8, 5, and 3 demonstrating the best binding energies. Subsequent MD simulation analyses indicated that all five compound formed stable complexes after 100 ns MD simulation. Consequently, these compounds hold promise as potential α‐amylase inhibitors pending successful clinical validation.

show abstract

Pyridazine Derivatives as New Antidiabetic Agents: Synthesis, In‐Vitro α‐Amylase Inhibitory Activity, Molecular Docking and Molecular Dynamics Simulations Studies

Boukharsa,

Alhaji Isa,

Sayah

et al. 2024

ChemistrySelect

View full text Add to dashboard Cite

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Synthesis and In-Vitro Antimycobacterial Evaluation of 4-Arylidene-2-Phenyl-6-(Aryl)-4,5-Dihydropyridazin-3(2H)-One Derivatives

Cited by 1 publication

References 43 publications

Pyridazine Derivatives as New Antidiabetic Agents: Synthesis, In‐Vitro α‐Amylase Inhibitory Activity, Molecular Docking and Molecular Dynamics Simulations Studies

Pyridazine Derivatives as New Antidiabetic Agents: Synthesis, In‐Vitro α‐Amylase Inhibitory Activity, Molecular Docking and Molecular Dynamics Simulations Studies

Contact Info

Product

Resources

About