Efficient approach to acyloxymethyl esters of nalidixic acid and in vitro evaluation as intra-ocular prodrugs |
| |
Authors: | Azéma Joëlle Guidetti Brigitte Malet-Martino Myriam Martino Robert Roques Christine |
| |
Affiliation: | Groupe de RMN Biomédicale, Laboratoire de Synthèse et Physicochimie de Molécules d'Intérêt Biologique, UMR CNRS 5068, Université Paul Sabatier, 118 route de Narbonne, 31062 Toulouse cedex 9, France. |
| |
Abstract: | Various alkylcarbonyloxymethyl esters of nalidixic acid ranging from 3 to 15 carbon units in the pro-moiety have been prepared and assessed as potential prodrugs. Their chromatographic retention factors k', silicone oil solubilities and in vitro conversion to nalidixic acid by a commercial esterase were determined together with their in vitro antimicrobial activity and cytotoxicity. The preliminary results suggest that silicone oil may have potential for the intra-ocular delivery of antibacterial compounds. Moreover, the in vitro release rate can be controlled by the lipophilicity of the prodrug. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|