131933-60-3Relevant academic research and scientific papers
Structure-activity relationship for enhancement of paracellular permeability across Caco-2 cell monolayers by 3-alkylamido-2-alkoxypropylphosphocholines
Ouyang, Hui,Morris-Natschke, Susan L.,Ishaq, Khalid S.,Ward, Peter,Liu, Dongzhou,Leonard, Sarah,Thakker, Dhiren R.
, p. 2857 - 2866 (2007/10/03)
Paracellular permeability enhancers have been used to improve the oral bioavailability of hydrophilic drugs; however, the mechanism of action of many enhancers is poorly understood. In this study, highly potent enhancers of paracellular permeability were
Structure-activity relationships for enhancement of paracellular permeability by 2-alkoxy-3-alkylamidopropylphosphocholines across Caco-2 cell monolayers
Liu, Dong-Zhou,Morris-Natschke, Susan L.,Kucera, Louis S.,Ishaq, Khalid S.,Thakker, Dhiren R.
, p. 1169 - 1174 (2007/10/03)
The oral route is the preferred route of delivery for a large number of drug molecules. However, the intestinal epithelium presents a formidable barrier for delivery of drugs into systemic circulation. Phospholipids are among compounds that enhance the ab
In Vitro Evaluation of Phosphocholine and Quaternary Ammonium Containing Lipids as Novel Anti-HIV Agents
Meyer, Karen L.,Marasco, Canio J.,Morris-Natschke, Susan L.,Ishaq, Khalid S.,Piantadosi, Claude,Kucera, Louis S.
, p. 1377 - 1383 (2007/10/02)
A series of synthetic lipids containing a two- or three-carbon backbone substituted with a thio, oxy, or amidoalkyl functionality and either a phosphocholine or quaternary ammonium moiety was evaluated as potential anti-HIV-1 agents.Several analogues were identified as possessing activity with the most promising compound being rac-3-octadecanamido-2-ethoxypropylphosphocholine (8).Compound 8 exhibited an IC50 for the inhibition of plaque formation of 0.16 μM wich was 84-fold lower than the IC50 value determined for CEM-SS cell growth inhibition.Initial mechanistic studies have indicated that these compounds, unlike AZT, are not reverse transcriptase (RT) inhibitors, but instead appear to inhibit a late step in HIV replication involving virus assembly and infectious virus production.Since these lipids are acting via a different mechanism, they represent an alternative approach to the chemotherapeutic treatment of AIDS as well as candidates for combination therapy with AZT.
