Aryl and Heteroaryl Phenylthiazoles for Enhanced Antimicrobial Activity Against Multidrug-Resistant Pathogens | ||||
| Azhar International Journal of Pharmaceutical and Medical Sciences | ||||
| Article 16, Volume 5, Issue 1, January 2025, Page 193-201 PDF (632.33 K) | ||||
| Document Type: Original research articles | ||||
| DOI: 10.21608/aijpms.2024.250852.1242 | ||||
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| Authors | ||||
Mariam Omara   1; Mohamed Hagras 2; Marwa T Sarg 1; Abdelrahman S Mayhoub2, 3
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| 1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt. | ||||
| 2Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt. | ||||
| 3Nanoscience Program, University of Science and Technology, Zewail City of Science and Technology, Giza, Egypt. | ||||
| Abstract | ||||
| The Phenylthiazole scaffold has been reported to exhibit an outstanding and promising antibacterial activity against a wide range of Gram positive multidrug-resistant bacteria, especially, staphylococci. According to the structure-activity relationship (SAR) a guanidine hydrophilic head moiety and a lipophilic tail moiety have been identified as crucial structural characteristics. In this study, the lipophilic component was investigated deeply through the synthesis of eight compounds using both direct and in situ Suzuki miyaura cross coupling reaction. Notably, compound 8d has demonstrated a promising MIC values against superbugs, including MRSA USA300, C. difficile, TolC Mutant E.coli, N. gonorrheae 181, and wild type C. albicans. These microbiological findings suggest that compound 8d holds a potential activity as an effective antibiotic against these challenging pathogens. Further research and development studies of this unique class of antibiotics possibly will lead to the discovery of new scaffolds and nucleus, hopefully used as a treatment for multidrug-resistant bacterial and fungal infections. | ||||
| Keywords | ||||
| Antimicrobial resistance; Methicillin-resistant Staphylococcus aureus; Suzuki cross-coupling; Phenylthiazoles; Minimum inhibitory concentration | ||||
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