Halogenation of Drugs Enhances Membrane Binding and Permeation (original) (raw)

The study investigates the impact of halogenation on the membrane binding and permeation of drugs, specifically focusing on chlorinated and fluorinated phenothiazine analogues. By substituting hydrogen with chlorine or trifluoromethyl groups at specific positions in the chemical structure, the research quantifies changes in the lipid-water partition coefficients and permeability coefficients. Results indicate significant enhancements in both partitioning into lipid membranes and permeability through biological membranes, demonstrating the effectiveness of halogen substitutions in improving drug delivery.