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.
Mancy, A. (2019). SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES. Al-Azhar Journal of Pharmaceutical Sciences, 60(2), 43-50. doi: 10.21608/ajps.2019.70236
MLA
Ahmed Mancy. "SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES". Al-Azhar Journal of Pharmaceutical Sciences, 60, 2, 2019, 43-50. doi: 10.21608/ajps.2019.70236
HARVARD
Mancy, A. (2019). 'SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES', Al-Azhar Journal of Pharmaceutical Sciences, 60(2), pp. 43-50. doi: 10.21608/ajps.2019.70236
VANCOUVER
Mancy, A. SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES. Al-Azhar Journal of Pharmaceutical Sciences, 2019; 60(2): 43-50. doi: 10.21608/ajps.2019.70236
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