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dc.contributor.authorKaraman, Rafik
dc.date.accessioned2018-09-08T13:49:21Z
dc.date.available2018-09-08T13:49:21Z
dc.date.issued2013-02-19
dc.identifier.issn0948-5023
dc.identifier.urihttps://dspace.alquds.edu/handle/20.500.12213/859
dc.description.abstractDFT calculations for the acid-catalyzed hydrolysis of several maleamic acid amide derivatives revealed that the reaction rate-limiting step is determined on the nature of the amine leaving group. Further, it was established that when the amine leaving group was a secondary amine, acyclovir or cefuroxime moiety the tetrahedral intermediate formation was the rate-limiting step such as in the cases of acyclovir ProD 1- ProD 4 and cefuroxime ProD 1- ProD 4. In addition, the linear correlation between the calculated and experimental rates provided a credible basis for designing prodrugs for masking bitter taste of the corresponding parental drugs which have the potential to release the parent drug in a sustained release fashion. For example, based on the DFT calculated rates the predicted t1/2 (a time needed for 50 % of the reactant to be hydrolyzed to products) for cefuroxime prodrugs, cefuroxime ProD 1- ProD 4, were 12 min, 18 min, 200 min and 123 min, respectively.en_US
dc.language.isoen_USen_US
dc.publisherSpringer-Verlagen_US
dc.subjectAntibacterial prodrugsen_US
dc.subjectCefuroxime prodrugsen_US
dc.subjectDFTcalculationsen_US
dc.subjectIntramolecular amide hydrolysisen_US
dc.subjectMaleamic acid amidesen_US
dc.subjectMasking bitter tasteen_US
dc.titleProdrugs for Masking Bitter Taste of Antibacterial Drugs - A Computational Approachen_US
dc.typeArticleen_US


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