SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS
Atwa, S., Hagras, M., Mayhoub, A., Elsebaei, M. (2024). SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS. EKB Journal Management System, 69(1), 108-129. doi: 10.21608/ajps.2024.360406
Saeed S Atwa; Mohamed Hagras; Abdelrahman S Mayhoub; Mohamed Elsebaei. "SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS". EKB Journal Management System, 69, 1, 2024, 108-129. doi: 10.21608/ajps.2024.360406
Atwa, S., Hagras, M., Mayhoub, A., Elsebaei, M. (2024). 'SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS', EKB Journal Management System, 69(1), pp. 108-129. doi: 10.21608/ajps.2024.360406
Atwa, S., Hagras, M., Mayhoub, A., Elsebaei, M. SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS. EKB Journal Management System, 2024; 69(1): 108-129. doi: 10.21608/ajps.2024.360406

SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS

Al-Azhar Journal of Pharmaceutical Sciences
Volume 69, Issue 1, March 2024, Page 108-129  XML PDF (1.53 MB)
Document Type: Original Article
DOI: 10.21608/ajps.2024.360406
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Authors
Saeed S Atwa1; Mohamed Hagras1; Abdelrahman S Mayhoub1, 2; Mohamed Elsebaei email 3
1Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt
2Nanoscience Program, University of Science and Technology, Zewail City of Science and Technology, Giza, Egypt
3Department of Pharmaceutical Organic Chemistry, College of Pharmacy(boys), Al-Azhar University, Cairo 11884, Egypt.
Abstract
Antibiotic resistance is a growing global health threat and requires extensive research to combat this urgent problem. Phenylthiazoles, known for their diverse biological activities including anthelmintic, insecticidal, and antimicrobial properties, have recently gained particular attention as potential anti-MRSA lead compounds. This class of compounds is an established pharmacophore for the development of new antibacterial agents, particularly against multidrug-resistant bacteria such as MRSA, a notorious pathogen resistant to most first-line antibiotics. In-depth structure-activity relationship (SAR) studies of phenylthiazoles revealed two key features critical to their antibacterial activity: a nitrogen-containing head and a lipophilic tail. In this study, we aimed to reduce the lipophilicity of phenylthiazoles and improve their overall physicochemical and pharmacokinetic profiles by synthesizing a new series bearing primary amines at the phenyl-4 position. Notably, compounds 5m exhibited bactericidal activity against MRSA, exhibiting a minimum inhibitory concentration (MIC) of only 8 µg/mL against the prevalent MRSA strain USA300.
Keywords
Antibiotic resistance; Phenylthiazole; anti-MRSA
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