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245 1 0 _aSynthesis of halogenated azo-aspirin analogues from natural product derivatives as the potential antibacterial agents.
490 0 _vNatural Product Research, 33(24), p.3507-3514, 2019
520 3 _aChemical modification of medicines from natural product-based molecules has become of interest in recent years. In this study, a series of halogenated azo derivatives 1a-d were synthesised via coupling reaction, followed by Steglich esterification with aspirin (a natural product derivative)to form azo derivatives 2a-d. While, halogenated azo-aspirin 3a-d were synthesised via direct coupling reaction of aspirin and diazonium salt. Bacteriostatic activity was demonstrated against E. coli and S. aureus via turbidimetric kinetic method. Compound 3a-d showed excellent antibacterial activities against E. coli (MIC 75-94 ppm)and S. aureus (MIC 64-89 ppm)compared to ampicillin (MIC 93 and 124 ppm respectively), followed by 1a-d and 2a-d. The presence of reactive groups of -OH, N=N, C=O and halogens significantly contribute excellent interaction towards E. coli and S. aureus. Molecular dockings analysis of 3a against MIaC protein showed binding free energy of ?7.2 kcal/mol (E. coli)and ?6.6 kcal/mol (S. aureus).
650 1 4 _aASPIRIN
650 1 4 _aAZO
650 1 4 _aTURBIDIMETRIC
650 1 4 _aCHEMICAL MODIFICATION
650 1 4 _aANTIBACTERIAL
700 1 2 _aNgaini, Z.
700 1 2 _aMortadza, N. A.
856 4 0 _uhttps://drive.google.com/file/d/1vkicNPGNCMHIku1F02TYgy9I_Tlo6gQe/view?usp=drivesdk
_zPara ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx
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