Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives
Rezk, M., Wasfy, A., Behalo, M., El-kalyoubi, S., Aly, A. (2025). Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives. EKB Journal Management System, (), -. doi: 10.21608/ejchem.2025.361774.11447
Marwa M. Rezk; A. A. F. Wasfy; Mohamed S. Behalo; Samar El-kalyoubi; Aly A. Aly. "Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives". EKB Journal Management System, , , 2025, -. doi: 10.21608/ejchem.2025.361774.11447
Rezk, M., Wasfy, A., Behalo, M., El-kalyoubi, S., Aly, A. (2025). 'Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives', EKB Journal Management System, (), pp. -. doi: 10.21608/ejchem.2025.361774.11447
Rezk, M., Wasfy, A., Behalo, M., El-kalyoubi, S., Aly, A. Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives. EKB Journal Management System, 2025; (): -. doi: 10.21608/ejchem.2025.361774.11447

Synthesis, Antimicrobial Activity and Molecular Docking of Novel Series of Phthalazine Derivatives

Egyptian Journal of Chemistry
Articles in Press, Accepted Manuscript, Available Online from 13 May 2025  XML
Document Type: Original Article
DOI: 10.21608/ejchem.2025.361774.11447
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Authors
Marwa M. Rezk email 1; A. A. F. Wasfyorcid 1; Mohamed S. Behaloorcid 1; Samar El-kalyoubi2; Aly A. Alyorcid 3
1Benha University, Faculty of Science, Chemistry Department, Egypt
2Port Said University, Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, Egypt
3Chemistry Department, Faculty of Science, Benha University, Benha, Egypt
Abstract
A straightforward and effective method for synthesizing phthalazine derivatives was developed through the reaction of 1-(4-(4-chlorophthalazin-1-yl)phenyl]-pyrrolidine-2,5-dione (3), a key precursor, with various nucleophiles containing carbon, nitrogen, oxygen, and sulfur. The structures of all synthesized compounds were verified through elemental analysis and spectral data. Furthermore, certain derivatives were assessed for their antibacterial and antifungal activities and compared with standard drugs. Among them, compounds 4, 14a, 15, and 18 demonstrated antimicrobial activity, positioning them as promising candidates for therapeutic use. In vitro testing demonstrated their potent efficacy against bacterial strains (Escherichia Coli, Staphylococcus Aureus) and fungal pathogens (Aspergillus niger), indicating broad-spectrum antimicrobial potential. Molecular docking analyses supported these findings, revealing strong binding interactions with key microbial enzymes, which aligns with their observed inhibitory effects. Combining potent antimicrobial activity and favorable pharmacokinetic characteristics, these compounds emerge as promising leads for the development of multitarget drugs targeting infectious diseases.
Keywords
Phthalazin-1-(2H)-one; Chlorophthalazine; Pyrrolidine-2; 5-dione; A antimicrobial activity; Molecular docking
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