This project deals with the design, synthesis, pharmacological evaluations, and computational studies of non-competitive antagonists of the NMDA receptor. This application is mainly to synthesize compounds that are derived from PCP, which is itself a non-competitive antagonist of the NMDA receptor. The hypothesis behind this project is that appropriately substituted fluorine and hydroxy groups on the aromatic ring of PCP and its rigid analogs will lead to compounds that are selective for the non-competitive sites on NMDA receptors that will not significantly bind to sigma receptors. A corollary to this hypothesis is that a compound that is selective for NMDA receptors and which binds poorly to sigma receptors will not have psychotic effects.
| Ates-Alagoz, Zeynep; Sun, Shengguo; Wallach, Jason et al. (2011) Syntheses and pharmacological evaluations of novel N-substituted bicyclo-heptane-2-amines at N-methyl-D-aspartate receptors. Chem Biol Drug Des 78:25-32 |
| Buyukbingol, Erdem; Sisman, Arzu; Akyildiz, Murat et al. (2007) Adaptive neuro-fuzzy inference system (ANFIS): a new approach to predictive modeling in QSAR applications: a study of neuro-fuzzy modeling of PCP-based NMDA receptor antagonists. Bioorg Med Chem 15:4265-82 |
| Gurkan, A Selen; Karabay, Arzu; Buyukbingol, Zeliha et al. (2005) Syntheses of novel indole lipoic acid derivatives and their antioxidant effects on lipid peroxidation. Arch Pharm (Weinheim) 338:67-73 |
| El-Gendy, Ahmed M; Adejare, Adeboye (2004) Membrane permeability related physicochemical properties of a novel gamma-secretase inhibitor. Int J Pharm 280:47-55 |
