SYNTHESIS OF SOME NEW AZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Volume 69, Issue 1, March 2024, Pages 108-129 PDF (1.53 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2024.360406 | ||
| Authors | ||
| Saeed S Atwa1; Mohamed Hagras1; Abdelrahman S Mayhoub1, 2; Mohamed Elsebaei* 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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