Synthesis of Dihydropyridine Prodrugs with Expected Enhancement of brain Delivery | ||
Journal of University of Babylon | ||
Article 1, Volume 20, Issue 2, June 2012, Pages 605-617 | ||
Authors | ||
Ahlam Jamil Qasir; Dunia Lafta Mhamad | ||
Abstract | ||
Recently non-steroidal anti-inflammatory drugs (NSAIDs) have been proposed to prevent or to cure Alzheimer’s disease. In this respect, we synthesized new potential prodrugs of several NSAIDs in order to increase their access to the brain. The carboxylic group of NSAIDs was attached to the 1,4-dihydro-1-methylpyridine-3-carboxylate moiety, which acts as a carrier, via an amino acid bridge, according to the chemical delivery approach developed by Bodor.In this study new analogues were synthesized by insertion D- Threonine moiety using esterification method then linked to nicotinic acid by conventional solution method using DCC as coupling reagent all prodrugs were more lipophilic when compared to their corresponding parent compounds and consequently a better blood brain barrier (BBB) penetration is hypothesised the analogues were purified and monitered by TLC , melting point , and IR spectrophotometer FT.IR 8400 was achieved and CHNS analysis. | ||
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