SYNTHESIS OF SOME NEW PYRAZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS | ||||
| Al-Azhar Journal of Pharmaceutical Sciences | ||||
| Volume 70, Issue 2, September 2024, Page 120-138 PDF (1.17 MB) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajps.2025.429937 | ||||
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| Authors | ||||
Mohamed Elsebaei  1; Ahmed A. Nasser2; Sherif F. Hammad3; Abdelrahman S. Mayhoub2
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| 1Department of Pharmaceutical Organic Chemistry, College of Pharmacy(boys), Al-Azhar University, Cairo 11884, Egypt. | ||||
| 2Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt. &University of Science and Technology, Nanoscience Program, Zewail City of Science and Technology, October Gardens, 6th of October, Giza 12578, Egypt. | ||||
| 3Basic and Applied Sciences Institute, Egypt-Japan University of Science and Technology (E-JUST), New Borg El-Arab City 21934, Alexandria, Egypt. | ||||
| Abstract | ||||
| Small organic phenylpyrazole scaffolds with high lipophilic properties are often associated with poor physicochemical properties, leading to more off-target actions and lower chances of full clinical trials. Therefore, we targeted the lipophilic tail of metabolically stable alkynylphenylpyrazole derivatives that exhibit remarkably high lipophilic properties and introduced a cyclic amine to improve their physicochemical characteristics. Alkynyl derivatives with 4-membered rings were the only ones that exhibited significant antibacterial activity. The azetidine moiety-containing compound 8 showed moderate antibacterial activity against MRSA. It significantly enhanced the water solubility and pharmacokinetic profile with an increase in the half-life and the time during which its plasma concentration was above its minimum inhibitory concentration against MRSA. The pharmacokinetic properties of the new series were successfully improved while the biological activity of the compounds against MRSA was maintained by the modifications of the alkynylphenylpyrazoles described here. | ||||
| Keywords | ||||
| antibiotic resistance; MDR-bacteria; MRSA; cyclic amine; Sonogashira cross-coupling | ||||
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