Piperidinecarboxamides with potential CNS and cardiovascular properties.
Several 1- and 2-(2-phenylethyl)piperidinecarboxamides were prepared and subjected to preliminary pharmacological studies. Moderate to strong activity by several compounds was observed in modified dopa potentiation tests in mice.
Chapter 2. Antidepressives and Stimulants
Publisher Summary This chapter discusses the biochemistry and pharmacology of antidepressives and stimulants. The synthesis and pharmacological evaluation of numerous potential antidepressives are presented. An amitriptyline derivative, exhibited a pharmacological profile similar to that of the parent. Antidepressive and antianxiety properties were also noted for a monomethyl analog. A dibenzthiepin, dothiepin, was superior to amitriptyline in a double blind comparison for the treatment of depression. Amoxapine, a dibenzoxazepine, although devoid of anticholinergic properties, produced imipramine-like activity in animals. Structure versus anti-depressive activity relationships were reported for a series of phenothiazines and related compounds bearing a carbocyclic basic side chain. The phenothiazines with antidepressive actions included the l-chloro-analog of chlorpromazine, which produced imipramine-like actions in mice and rats, and the azaphenothiazine-10-thiolcarboxylate, which induced antidepressive-like symptoms in mice. The antidepressive effects of phenothiazine derivatives with 1- or α-substituents may be associated with the steric influence of these groups in interfering with attainment of a nearly flat conformation by the tricyclic system.
Identification of Dihydroxy Aromatic Compounds in a Low-Temperature Pyrolysis Coal Tar by Gas Chromatography−Mass Spectrometry (GC−MS) and Fourier Transform Ion Cyclotron Resonance Mass Spectrometry (FT-ICR MS)
Dihydroxy aromatics in coal tar undergo rapid coupling reactions with each other and with some coal-derived species during coal pyrolysis and liquefaction. However, only limited information on the structure of dihydroxy aromatics is known. In this study, Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS) and gas chromatography−mass spectrometry (GC−MS) were used to characterize the dihydroxy aromatics in a low-temperature pyrolyzed coal tar and its distillate and residue fractions. Negative-ion electrospray ionization (ESI) FT-ICR MS spectra of coal-tar-derived samples had low molecular masses and narrow mass ranges. Negative-ion ESI is extremely selective for the dihydroxy aromatics present in coal tar. The O2 class species had the highest ion intensity among the species in the negative-ion FT-ICR mass spectrum for each sample. Dihydroxy compounds with an aromatic core structure of benzene, indan, biphenyl (and/or acenaphthene), and naphthalene were identified in the distillate fract...