SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES | ||||
| Al-Azhar Journal of Pharmaceutical Sciences | ||||
| Article 4, Volume 60, Issue 2, September and October 2019, Page 43-50 PDF (437.19 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajps.2019.70236 | ||||
 View on SCiNiTO | ||||
| Author | ||||
Ahmed Mancy 
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| Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt | ||||
| Abstract | ||||
| Antibiotics are a cornerstone of medical treatment for various bacterial infections and are prescribed at a rate that exceeds the limit of prescribing. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci.The structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the acetylene part in analogues with a prolonged half-life, while the cyclic nitrogenous extention revealed the most potent analogue. In the current work, advantageous moieties have been tethered together to produce a new scaffold of phenylthiazole with the objective of promoting new scaffold enhancing both antimicrobial resistance activity and drug-like properties. Among the tested phenylthiazoles, compounds 14 and 16 were found to exert a bactericidal activity against MRSA. The pharmacokinetic profile of compound 15 was significantly enhanced against biofilm of the bacteria. | ||||
| Keywords | ||||
| Phenylthiazole; Antimicrobial resistance; Improve solubility; Infections; Acetylene part | ||||
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