piperidine/nekroos

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Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.

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A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized. Their structure-activity relationships, against tumor necrosis factor-alpha (TACE) and matrix metalloproteinase (MMP) inhibitor activities, are presented by

BW1003C87 and NBQX but not CGS19755 reduce glutamate release and cerebral ischemic necrosis.

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This study examines the relationship between the concentration of extracellular glutamate released during 30 min of forebrain ischemia, and the subsequent development of ischemic neural necrosis, in the presence of three agents which act at distinct sites on the glutamatergic synapse: a presynaptic

A spin decay assay for tumor necrosis factor cytotoxicity.

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Tumor necrosis factor (TNF) is believed to elicit its response primarily by an oxidative process. We present a sensitive biophysical assay system to monitor TNF-induced cell killing by electron paramagnetic resonance (EPR) spectroscopy using the spin label 2,2,6,6-tetramethyl-1-piperidine-n-oxyl

Photochemical and phototoxic properties of ethyl 1,4-dihydro-8-nitro-4-oxoquinoline-3-carboxylate, a new quinoline derivative.

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The present study demonstrates photoinduced generation of superoxide radical anion and singlet oxygen upon UVA irradiation of ethyl 1,4-dihydro-8-nitro-4-oxoquinoline-3-carboxylate (DNQC), and its cytotoxic/phototoxic effects on murine leukemia L1210 cells. The formation of reactive oxygen species

TCP enhances the survival of human fetal spinal cord cells in culture.

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Dissociated cell cultures were prepared from human spinal cords of 7-10-week-old fetuses. After 10 weeks progressive neuronal necrosis was observed in controls whereas N/1-(2-thienyl)cyclohexyl/piperidine (TCP) enhanced the survival time of the cells. After 21 weeks the number of gamma-aminobutyric

beta-sitosterol among other secondary metabolites of Piper galeatum shows inhibition of TNFalpha-induced cell adhesion molecule expression on human endothelial cells.

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A phytochemical investigation of the stems of Piper galeatum yielded one novel amide, 1-(3'-hydroxy-5'-methoxycinnamoyl)-piperidine (5) along with four known compounds, i.e. beta-sitosterol (1), cyclostachine-A (2), piperine (3) and piperolein-B (4). The structures of all the five compounds,

Lesions of amygdala, pyriform cortex and other brain structures due to dipiperidinoethane intoxication.

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Single doses of dipiperidinoethane (DPE) produced symmetrical necrosis in pyriform cortex, amygdala and other areas of gray matter in rats, mice and gerbils. The necrosis was detectable in 10 hours and fully developed in 24 hours. Its distribution and severity were not influenced by carotid artery

Cytostatic in vitro effects of DTCM-glutarimide on bladder carcinoma cells.

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Bladder cancer is a common malignancy worldwide. Despite the increased use of cisplatin-based combination therapy, the outcomes for patients with advanced disease remain poor. Recently, altered activation of the PI3K/ Akt/mTOR pathway has been associated with reduced patient survival and advanced

Pharmacology of new glutarimide compounds.

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New glutarimide compounds were synthesized by incorporating piperidine (compounds 1 to 7), diethylamine (8 and 9), morpholine moities (10 to 13), and alkyl derivatives of 3,5 dicyanoglutarimide (14 to 20) at position -1 of the nitrogen atom. Only compounds 1 to 7 at a dose of 8 mg/kg i.p. caused

NTP Toxicology and Carcinogenesis Studies of Pyridine (CAS No. 110-86-1) in F344/N Rats, Wistar Rats, and B6C3F1 Mice (Drinking Water Studies).

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Pyridine is used as a denaturant in alcohol and anti freeze mixtures, as a solvent for paint, rubber, and polycarbonate resins, and as an intermediate in the manufacture of insecticides, herbicides, and fungicides. It is used in the production of piperidine, an intermediate in the manufacture of

Electrochemistry of norcocaine nitroxide and related compounds: implications for cocaine hepatotoxicity.

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Norcocaine nitroxide, a free radical metabolite of cocaine, displays a reversible one-electron cyclic voltammogram which is abolished by the addition of reduced glutathione. The corresponding nitrosonium ion was synthesized. It showed the same electrochemical characteristics as the nitroxide. The

Inhibition of monoacylglycerol lipase attenuates nonsteroidal anti-inflammatory drug-induced gastric hemorrhages in mice.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used analgesics, but can cause gastric and esophageal hemorrhages, erosion, and ulceration. The endogenous cannabinoid (endocannabinoid; eCB) system possesses several potential targets to reduce gastric inflammatory states, including

Quinazoline based α1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines.

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New α1-adrenoreceptor (α1-AR) antagonists related to prazosin and doxazosin were synthesized by replacing piperazine ring with (S)- or (R)-3-aminopiperidine. Binding studies indicated that the S configuration at the 3-C position of the piperidine ring is crucial for an optimal interaction of the

A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.

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Certain leukocytes release serine proteases that sustain inflammatory processes and cause disease conditions, such as asthma and chronic obstructive pulmonary disease. We identified beta-ketophosphonate 1 (JNJ-10311795; RWJ-355871) as a novel, potent dual inhibitor of neutrophil cathepsin G (K(i) =

Lenalidomide in an in vitro Dendritic Cell Model for Malignant Gliomas.

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Malignant gliomas are tumors with a very unfavorable prognosis. They are characterized by rapid proliferation and invasion in the surrounding healthy tissue. Complete resection of the tumor is still the most important therapeutic option. Despite a variety of therapy modifications in the last years,

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