SYNTHESIS AND EVALUATION OF NEW ARYLAZOLES DERIVATIVES AGAINST METHICILLIN RESISTANT BACTERIA | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 1, Volume 61, Issue 1, March 2020, Pages 1-11 PDF (722.08 K) | ||
| Document Type: Review Article | ||
| DOI: 10.21608/ajps.2020.86008 | ||
| Author | ||
| Mohamed Hannoun* | ||
| Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt | ||
| Abstract | ||
| In the previously reported arylthiazole antibiotics the lipophilic part of the n-butylphenyl moiety was replaced with naphthyl ring which improved its activity against Vancomycin resistant strains of Staphylococcus aureus. In the other hand, the incorporation of the C=N linker connecting the nitrogenous head with thiazole within an oxadiazole ring provided orally available analogs with relatively long half-life. New eight derivatives of 2-(thiazol-5-yl)-1,3,4-oxadiazole was synthesized by combining both structural modifications in one new scaffold to enhance the pharmacokinetic profile and antibacterial activities against malicious microbes, two of them is comparably potent as Vancomycin. | ||
| Keywords | ||
| Arylazoles; Antimicrobial; Oxadiazole; phenylthiazole | ||
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