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Studies on Antibacterial Action of Sulfonamide Drugs. III. Correlation of Drug Activity with Binding to Plasma Proteins
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References
1942
Year
Pharmaceutical ScienceBioorganic ChemistrySulfonamide DrugsAntimicrobial ChemotherapyPharmaceutical ChemistryDrug ResistanceDrug ActivityMedicinal ChemistryAntimicrobial ResistanceBiochemistryAntibacterial AgentAntimicrobial CompoundPlasma ProteinsPharmacologyQuantitative CorrelationNatural SciencesProtein-binding PowerMedicineDrug Discovery
The protein-binding power of 7 commonly employed sulfonamide drugs has been measured by dialysis experiments. A quantitative correlation has been demonstrated between the protein-binding tendency and the bacteriostatic activity of the 7 drugs. Alteration of the p-amino structure of the compounds failed to affect significantly the protein-binding power although it destroyed the antibacterial properties. The data presented here and in another publication by one of us support the recently advanced hypothesis that the anionic species of the sulfonamide molecule is the active component involved in the mechanism of bacteriostasis.