ArticleJournal of molecular modeling2013
Prodrugs for masking bitter taste of antibacterial drugs--a computational approach.
Article in Journal of molecular modeling, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Electrochemical Sensors as a Tool for Taste Perception in Pharmaceutical Products: Advances and Perspectives.Biosensors · 2026Review
- Crushing tablets or sprinkling capsules: Implications for clinical strategy and study performance based on BE studies of rivaroxaban and deferasirox.Clinical and translational science · 2024Review
- Mesoporous Silica Carrier-Based Composites for Taste-Masking of Bitter Drug: Fabrication and Palatability Evaluation.AAPS PharmSciTech · 2022Article
- Study on Masking the Bitterness of Chinese Medicine Decoction-Mate.Evidence-based complementary and alternative medicine : eCAM · 2022Article
- Inulin and Its Application in Drug Delivery.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Encapsulation of Active Pharmaceutical Ingredients in Lipid Micro/Nanoparticles for Oral Administration by Spray-Cooling.Pharmaceutics · 2021Review
- Enzyme Models-From Catalysis to Prodrugs.Molecules (Basel, Switzerland) · 2021Review
- Development and evaluation of taste masked dry syrup formulation of potassium chloride.AAPS open · 2019Article
- BitterSweetForest: A Random Forest Based Binary Classifier to Predict Bitterness and Sweetness of Chemical Compounds.Frontiers in chemistry · 2018Article
- Design, synthesis, and in vitro kinetics study of atenolol prodrugs for the use in aqueous formulations.TheScientificWorldJournal · 2014Article
- Computationally designed prodrugs of statins based on Kirby's enzyme model.Journal of molecular modeling · 2013Article
Corrections and comments
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Authors and funding
1 author.
Funding
No grant is acknowledged in the PubMed record.
Abstract
DFT 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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.