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Development of novel antibiotics derived from pyridazine: Synthesis, spectroscopic characterization, in vitro antimicrobial activity and molecular docking studies

Authors :
Mouad Lahyaoui
Mouad Filali
Khadija Benamar
Riham Sghyar
Kawtar Fikri-Benbrahim
Amal Haoudi
Ahmed Mazzah
Souad El khattabi
El Mestafa El Hadrami
Youssef Kandri Rodi
Nada Kheira Sebbar
Source :
Results in Chemistry, Vol 10, Iss , Pp 101699- (2024)
Publication Year :
2024
Publisher :
Elsevier, 2024.

Abstract

In light of the increasing antibiotic resistance, it is crucial to discover new antimicrobial medications. Pyridazines are frequently investigated in research for the development of new chemical entities with enhanced therapeutic properties. Their structure allows for significant flexibility in the attachment of various functional groups, which is essential for drug discovery.Our work focuses on synthesizing new pyridazine derivatives (7a, 7b, 7c and 7d) through coupling reactions with various amino esters. The structures of these compounds have been analyzed using spectroscopic measurements including 1H, 13C NMR, IR, and mass spectroscopy. The compounds showed positive effects against two bacterial strains: Escherichia coli: ATCC25922 and Staphylococcus aureus: CIP543154. Molecular docking results of the protein 7AZ5 indicated significant affinities with these molecules through hydrogen bonds. Compounds 7a and 7d demonstrated the highest binding energies and the best antimicrobial activity, suggesting their potential as a model for creating novel and potent antimicrobial compounds.

Details

Language :
English
ISSN :
22117156
Volume :
10
Issue :
101699-
Database :
Directory of Open Access Journals
Journal :
Results in Chemistry
Publication Type :
Academic Journal
Accession number :
edsdoj.5b994ed0f0544968934b5f2336db6465
Document Type :
article
Full Text :
https://doi.org/10.1016/j.rechem.2024.101699