The neurotoxic side effects observed for the neuroleptic agent haloperidol have been associated with its pyridinium metabolite. In a previous study, a silicon analog of haloperidol (sila-haloperidol) was synthesized, which contains a silicon atom instead of the carbon atom in the 4-position of the piperidine ring. In the present study, the phase I metabolism of sila-haloperidol and haloperidol ...

Following the discovery of a new series of anti-acetylcholinesterase (anti-AChE) inhibitors such as 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine (1), we reported that its rigid analogue, 1-benzyl-4-(2-isoindolin-2-ylethyl)piperidine (5), had more potent activity. We have extended the structure-activity relationship (SAR) study for the rigid analogue and found that the 2-isoindoline moiety in ...

Quantum chemical calculations have been performed for a number of siloxy derivatives of pyrrolidine and piperidine in an attempt to gauge the effect of the saturated ring on the SiON angle. Most derivatives of pyrrolidine had SiON angles comparable to those previously observed for substituted N,N-dimethylhydroxylamines. However, piperidine derivatives were predicted to have particularly narrow ...

The title compound, C28H32N2, (I), is one of a second generation of compounds designed and synthesized based on a very potent and selective α9α10 nicotinic acetyl-choline receptor antagonist ZZ161C {1,1'-[[1,1'-biphen-yl]-4,4'-diylbis(prop-2-yne-3,1-di-yl)]bis-(3,4-di-methyl-pyridin-1-ium) bromide}, which has shown analgesic effects in a chemotherapy-induced neuropathy animal model. Compound (I...

Background and Objective: N-Methyl-D-aspartate (NMDA) antagonists such as piperidines are the most important antiepileptic drugs. Considering the fact that piperidine derivatives such as phencyclidine (PCP) and its new derivative, 1-[1-(3-methoxyphenyl) (tetralyl)] piperidine (PCP1), have different potencies, the antiepileptic effects of mentioned drugs were investigated in the present study. M...

a series of 2-amino-4-aryl-3-cyano-7-(dimethylamino)-4 h -chromenes was synthesized by condensation of 3-(dimethylamino)phenol, an aromatic aldehyde and malonitrile in ethanol containing piperidine. the assignments of the structure of all synthesized compounds were based on spectral data (ir, mass and 1 h nmr). the cytotoxic activities of the synthesized compounds against six human tumor cell l...

The effects of local anesthetics were examined on a family of transiently expressed neuronal calcium channels. Fomocaine, a local anesthetic containing a morpholine ring, preferentially blocked (Y,~ channels (Ki = 100 PM), and had a lower affinity (3to 15fold) for (Y,~, (Y,~, and cz,c channels. Block was incompletely reversible, followed I:1 kinetics, and did not affect steady-state inactivatio...