Novel terpyridines as <i>Staphylococcus</i> <i>aureus</i> gyrase inhibitors: efficient synthesis and antibacterial assessment via solvent-drop grinding-Reference-Cited by-同舟云学术

Novel terpyridines as Staphylococcus aureus gyrase inhibitors: efficient synthesis and antibacterial assessment via solvent-drop grinding

Published:2024-02 Issue:3 Volume:16 Page:205-220
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Mohamed Mahmoud Abdalla¹²,Abouzied Amr Salah³⁴^ORCID,Reyad Amany⁵,Sayed Abdelsalam Zaki Magdi El⁶^ORCID,Abdelgawad Fathy Elsayed⁷^ORCID,Al-Humaidi Jehan Yahya⁸^ORCID,Gomha Sobhi Mohamed⁷⁹^ORCID

Affiliation:

1. Technology of Textile Department, Faculty of Technology and Education, Beni-Suef University, Beni-Suef, Egypt

2. Chemistry Department, Faculty of Science and Humanity study, Afif, Shaqra University, Saudi Arabia

3. Department of Pharmaceutical Chemistry, College of Pharmacy, University of Hail, Hail, 81442, Saudi Arabia

4. Department of Pharmaceutical Chemistry, National Organization for Drug Control & Research, Giza, 12311, Egypt

5. Botany Department, Faculty of Science, Fayoum University, Fayoum, 63514, Egypt

6. Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University, Riyadh, 11623, Saudi Arabia

7. Department of Chemistry, Faculty of Science, Islamic University of Madinah, Madinah 42351, Saudi Arabia

8. Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, P.O. BOX 84428, Riyadh 11671, Saudi Arabia

9. Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt

Abstract

Aim: This study was designed to synthesize a novel series of terpyridines with potential antibacterial properties, targeting multidrug resistance. Materials & methods: Terpyridines (4a–h and 6a–c) were synthesized via a one-pot multicomponent reaction using 2,6-diacetylpyridines, benzaldehyde derivatives and malononitrile or ethyl 2-cyanoacetate. The reactions, conducted under grinding conditions with glacial acetic acid, produced high-yield compounds, confirmed by spectroscopic data. Results: The synthesized terpyridines exhibited potent antibacterial activity. Notably, compounds 4d and 4h demonstrated significant inhibition zones against Staphylococcus aureus and Bacillus subtilis, outperforming ciprofloxacin. Conclusion: Molecular docking studies highlighted compounds 4d, 4h and 6c as having strong binding affinity to DNA gyrase B, correlating with their robust antibacterial activity, suggesting their potential as effective agents against multidrug-resistant bacterial strains.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2023-0278

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