Phencyclidine (PCP) binds inside of N-methyl-D-aspartate (NMDA) receptors of neurons and blocks ion flux. Over-stimulation of NMDA receptors during states of ischaemia, such as stroke, can cause membrane potential collapse by allowing too much Ca2+ entry. The designed compounds, using PCP as lead compound, are expected to act as noncompetitive NMDA receptor antagonist, preventing excitotoxicity even in the presence of excitants. The purpose of this study was to synthesize and evaluate novel target compounds, and pharmaceutical profiling of one compound was also carried out. All of the target compounds were synthesized in good yields via four steps, and the net yields varied from 10 to 50%. Compounds were characterized by NMR, MS, and other spectra. Several of the target compounds were evaluated as anticonvulsants using the maximal electroshock (MES) test. One of the compounds exhibited significant anticonvulsant properties at therapeutic doses and minimal side effects. In vitro binding studies showed anticonvulsant activity was from blocking NMDA receptor. The pKa, log P, and intrinsic solubility of this compound were evaluated as part of pharmaceutical profiling studies.