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At least 1,099 records · Page 61Linked to original sources
PubMed2006

Highly regio- and chemoselective ring opening of oxa-bridged piperidinones toward functionalized furanones and piperidines.

Lewis acid mediated competitive ring-opening reactions of N-tosyl-substituted oxa-bridged piperidinone ring systems are demonstrated. A majority of the Lewis acids furnished the regio- and chemoselective reductive ring opening at the C(1)-N bond, whereas TiCl(4) furnished at the C(1)-O bond in the presence of triethylsilane, affording functionalized furanones and dihydroxypiperidines, respectively. [reaction: see text]

Journal Article↗
PubMed1991

Endocrine, pharmacokinetic and clinical studies of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione ('pyridoglutethimide') in postmenopausal breast cancer patients.

The aromatase inhibitor, 'pyridoglutethimide' (PyG), has been shown previously to suppress serum oestrogen levels in postmenopausal breast cancer patients and to achieve clinical responses at a dose of 500 mg twice daily (b.d.). This report gives the results of a detailed pharmacokinetic and endocrine study of PyG in ten patients. Four doses were tested at intervals of 2 weeks in the following order: 200 mg b.d., 400 mg b.d., 800 mg b.d., 1200 mg b.d. Concentration-time profiles of serum levels of PyG were curvilinear in all patients probably reflecting a saturation of metabolic enzymes. During repeat-dosing metabolism was enhanced approximately 2-fold. Plasma levels of oestradiol were significantly suppressed by the lowest dose of PyG. Although higher doses appeared to achieve greater suppression this was not statistically significant in this small group of patients. There were no significant effects at any dose on the serum levels of cortisol, aldosterone, luteinising hormone, follicle stimulating hormone, prolactin, sex hormone binding globulin or thyroid stimulating hormone. There was a dose-related increase in 17 alpha-hydroxyprogesterone levels and a dose-related decrease in levels of dehydroepiandrosterone sulphate (DHAS). The androgens DHA, testosterone and androstenedione also were significantly suppressed with at least one of the doses of PyG. Synacthen tests did not support these changes being a result of inhibition of 17,20 lyase. It is possible that they are due to enhanced clearance of DHAS. Two patients experienced no toxicity throughout the study, whilst a total of four patients were withdrawn because of side-effects: one at 400 mg b.d., two at 800 mg b.d., and one at 1200 mg b.d. The most frequent side-effects were nausea and lethargy. One patient showed an objective response to treatment.

Aged↗
PubMed2001

cis-Tetracarbonyl[4-fluorophenyl)-diphenylphosphine-P](piperidine-N)-molybdenum(0).

The title molecule, [Mo[P(C6H5)2(C6H4F)](HNC5H10)(CO)4] or [Mo(C18H14FP)(C5H11N)(CO)4], has irregular octahedral geometry about the Mo atom. The molecules form a complicated hydrogen-bonded network comprising C-H...O, C-H...F and C-H...pi hydrogen bonds and pi-pi interactions. The C-H...pi and pi-pi interactions form chains containing C-H...pi/pi-pi dimers linked via C-H...pi interactions and the chains are linked into a three-dimensional network via C-H...O and C-H...F hydrogen bonds.

Journal Article↗
PubMed2003

Bis[(2,2-dimethyl-1,3-propanediamine-kappa2N,N')(piperidine-2-carboxylato-kappa2N,O)platinum(II)] sulfate.

The title compound, [Pt(C(6)H(10)NO(2))(C(5)H(14)N(2))](2)(SO(4)), crystallizes with two cations in the asymmetric unit. The two complex cations, which have a square-planar Pt(II) coordination, are chemically identical but differ slightly in the conformations of their amine groups. A neutral complex, viz. (2,2-dimethyl-1,3-propanediamine-kappa(2)N,N')bis(2-piperidinecarboxylato-kappaN)platinum(II), is shown to form in solution and to change rapidly into the title compound.

Journal Article↗
PubMed2006

{4(S)-(Piperidin-1-ylcarbonyl)-4-[3-(trifluoromethyl)phenylsulfonamido]butyl}guanidinium chloride: a model of a graftable thrombin inhibitor.

In the title compound, C18H27F3N5O3S+.Cl-, the guanidine group forms N-H...Cl hydrogen bonds, with four N...Cl distances in the range 3.164 (3)-3.337 (4) A. In the crystal packing, the cations are further linked by N-H...O and C-H...O interactions. The structure is compared with that of argatroban complexed with thrombin and is the subject of docking studies in the active site of thrombin.

Antithrombins↗
PubMed1960

Central vasomotor effects of a new ganglion-blocking agent--1: 2: 2: 6: 6-pentamethyl piperidine (pempidine).

The central vasomotor effects of pempidine were studied in dogs and cats anaesthetized with pentobarbitone sodium, and in spinal cats. Pempidine lowered the threshold of electrical stimulation of the medulla oblongata to evoke a pressor response when given intravenously to cats in a dose insufficient to block autonomic ganglia. Injection of a small dose into the cerebral ventricles of dogs produced an increase in the pressor responses to occlusion of the carotid artery and to electrical stimulation of the central end of the cut vagus. In the spinal cat small doses of pempidine, given either intravenously or intrathecally, augmented the rise in blood pressure resulting from compression of the spinal cord. Since all these effects were produced by pempidine in doses insufficient to cause ganglionic block, the observed effects are attributed to central facilitation of the vasomotor responses. Thus pempidine has a stimulant action on the spinal and supraspinal centres.

Animals↗
PubMed2006

Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors V. A series of new derivatives containing a spiro[imidazo[1,2-a]pyrazine-2(3H),4'-piperidin]-5(1H)-one scaffold.

We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved in a similar fashion to the N,O-spiro acetal synthesis. Consequently, FXa inhibitory activity was increased and more active compounds could be found (M58163: IC50 = 0.61 nM, M58169: IC50 = 0.58 nM). Additionally, the absolute configuration could be determined by X-ray crystallography analysis (M58169: (R)-config.).

Crystallography, X-Ray↗
PubMed1993

The metabolism of piperidine-type phenothiazine antipsychotic agents. III. Mesoridazine in dog, human and rat.

1. The metabolism of mesoridazine was studied in female rats (20 mg/kg, oral), female dogs (50 mg over 30 h, oral) and adult male volunteers (25 mg, oral). 2. Solvent extracts of urines from each species were directly analysed by h.p.l.c.-mass spectrometry with a plasmaspray interface. In the case of phenolic metabolites the urinary extracts were derivatized with a silylating reagent (with and without prior enzymic hydrolysis) prior to analysis. The structures of metabolites, with the exceptions of mesoridazine N-oxide and phenols, were confirmed by comparison of their chromatographic behaviours and mass spectra with those of authentic standards. 3. Compounds identified in the urine of all three species were mesoridazine, sulforidazine, mesoridazine ring sulphoxide, sulforidazine ring sulphoxide, N-desmethylmesoridazine ring sulphoxide, the lactam of sulforidazine ring sulphoxide and phenolic derivatives of mesoridazine and sulforidazine. Whereas the unconjugated phenolic metabolite of sulforidazine was present in urine of all three species, the conjugated form was identified only in dog and rat urines. Also, the unconjugated phenolic metabolite of mesoridazine was identified only in the urine of dog and human, but rat urine contained only the conjugated form. 4. Other metabolites found were: the lactam of mesoridazine (rat), the lactam of mesoridazine ring sulphoxide (rat and human), mesoridazine N-oxide (human) and sulforidazine N-oxide (dog and human). 5. Mesoridazine and six of its metabolites present in urines of human, rat and dog were quantified by a h.p.l.c.-u.v. method. The mean total excretion of measured analytes in human, rat and dog were 6.3, 2.6 and 29.1%, respectively. The excretion of the lactam of sulforidazine ring sulphoxide was greater in human (0.4%) and rat (0.2%) than dog (0.02%). Moreover, the urinary excretion of the lactam of mesoridazine ring sulphoxide in human and rat constituted 0.4% and 0.2%, respectively. Of the three lactams found in rat the lactam of mesoridazine was present in the least amount (0.05%). 6. Interspecies comparison of the lactam metabolites indicated that both qualitatively and quantitatively human more closely resembled rat than dog. On the other hand, N-oxide metabolites were detected in human and dog but not in rat.

Adult↗