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- Title
SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY EVALUATION OF NEW SULFAMETHOXAZOLE-PHOSPHATE ESTER PRODRUGS AND THEIR RELEASE AT DIFFERENT ACIDIC MEDIA.
- Authors
Eraibi, Fatima Abdulkareem; Hameed, Ayad Saadi
- Abstract
This research involved the preparation of three tri phosphate ester as prodrug carriers (F1 -F3 ), by reacting three equivalents of hydroxy benzaldehyde derivatives with one equivalent of POCl3 . Carriers compounds (F1 -F3 ) have been reacted with Sulfamethoxazole drug in the presence of acetic acid as a catalyst, to give (F4 -F6 ) prodrugs. Synthesized prodrugs with carriers were identified with C.H.N, IR and 1H-NMR techniques. The biological activity of (F4 ) prodrug and Sulfamethoxazole was performed against three types of bacteria (Escherichia coli), (Klebseilla pneumonia) and (Staphylococcus aureus). The preliminary obtained results indicated that prodrug (F4 ) has higher inhibition zone than Sulfamethoxazole. Drug release of prodrug (F4 ) has been tested in different pH media and according to the obtained data a proposed mechanism was investigated
- Subjects
SULFAMETHOXAZOLE; PHOSPHATE esters; PRODRUGS; ANTIBODY-directed enzyme prodrug therapy; ANTIBACTERIAL agents
- Publication
Biochemical & Cellular Archives, 2021, Vol 21, Issue 1, p433
- ISSN
0972-5075
- Publication type
Article