| abstract |
The present invention relates to prodrugs of positively charged non-steroidal anti-inflammatory drugs represented by the general formula (1, 2a, 2b, 2c or 2d) "structural formula 1, 2a, 2b, 2c or 2d". The compound represented by the general formula (1, 2a, 2b, 2c or 2d) "structural formula 1, 2a, 2b, 2c or 2d" can be prepared by reacting a metal salt or an organic base salt of a non-steroidal anti-inflammatory drug with an appropriate halide . The positively charged amino group in the prodrug greatly improves the solubility of the drug in water, and can also bind to the negative charge on the phosphate end group of the biofilm. Thus, the local concentration of the drug on the outside of the biofilm or skin will be high, thereby facilitating the diffusion of these prodrugs from areas of high concentration to areas of low concentration. This binding slightly perturbs the biofilm to make room for the lipid-soluble portion of the prodrug. When the molecules of the biofilm move, the biofilm is slightly squeezed due to the binding effect of the prodrug. When the amino group is not protonated, the amino group in the prodrug is separated from the phosphate end group of the biofilm, and the prodrug will completely enter the biofilm. |