Disease relevance of PYRROLIDINONE

• The in vitro potency of BAL 9141, a new pyrrolidinone cephalosporin, was tested against non-duplicate strains of anaerobic bacteria [1].
• OBJECTIVE: To investigate whether pyrrolidinone derivative (N2733), an inhibitor of nuclear factor (NF)-kappaB activation, improves altered metabolic and hemodynamic changes and organ dysfunctions caused by endotoxic shock [2].
• Optimization of pyrrolidinone based HIV protease inhibitors [3].
• The protective effects of BMY-21502 (1-[[1-[2-(trifluoromethyl)-4-pyrimidinyl]-4-piperidinyl]methyl]-2- pyrrolidinone) against cerebral anoxia were investigated using various models in mice, in comparison with those of other cerebroactive drugs [4].
• Pyrrolidinobenzoic acid inhibitors of influenza virus neuraminidase: modifications of essential pyrrolidinone ring substituents [5].

Psychiatry related information on PYRROLIDINONE

• Low nanomolar inhibition of BACE1, an enzyme implicated in the cascade of events leading to plaque formation in Alzheimer's disease, was found with a pyrrolidinone analogue [6].
• BMY 21502 is a novel pyrrolidinone nootropic with demonstrated ability to reverse electroconvulsively induced amnesia in rodents [7].

High impact information on PYRROLIDINONE

• We have produced a transgenic mouse (PV1TgL) that can only generate B lymphocytes with an Ig receptor specific for the synthetic polymer polyvinyl pyrrolidinone [8].
• Ancillary chemistry that involves thermal fragmentation of an iminobenzoxazine to a nitrile ylide and Me(2)AlSPh-mediated cyclization of oxime ether-ester 22 to pyrrolidinone 23 is also described [9].
• METHODS: In vivo measurements of GABA, homocarnosine, and pyrrolidinone were made of a 14-cm3 volume in the occipital cortex using 1H spectroscopy with a 2.1-Tesla magnetic resonance spectrometer and an 8-cm surface coil [10].
• In vitro activities of BAL9141, a novel broad-spectrum pyrrolidinone cephalosporin, against gram-negative nonfermenters [11].
• This work presents a high-throughput selected reaction monitoring LC-MS bioanalytical method for the determination of idoxifene, a selective estrogen receptor modulator, and its pyrrolidinone metabolite in clinical human plasma samples [12].

Chemical compound and disease context of PYRROLIDINONE

• 3. Some of the pyrrolidinone derivatives also prevent amnesia associated with inhibition of acetylcholine synthesis brought about by hemicholinium [13].
• The pyrrolidinone derivative aniracetam given orally immediately after acquisition of an inhibitory avoidance response reproducibly ameliorated scopolamine-induced amnesia in female rats in an extensive series of test sessions conducted over a 1-year period [14].

Biological context of PYRROLIDINONE

• The nitrosation characteristics of pyrrolidinone indicate its possible conversion to nitrosopyrrolidinone under conditions of the gastric tract [15].
• The effects of the substituted pyrrolidinone, BMY 21502, on the properties of cell membranes, synaptic transmission and synaptic plasticity, were assessed in area CA1 of hippocampal slices from the rat [16].
• Phenotype of B cells responding to the thymus-independent type-2 antigen polyvinyl pyrrolidinone [17].
• Biotransformation of a new pyrrolidinone cognition-enhancing agent: isolation and identification of metabolites in human urine [18].
• A pyrrolidinone derivative inhibits cytokine-induced iNOS expression and NF-kappaB activation by preventing phosphorylation and degradation of IkappaB-alpha [19].

Anatomical context of PYRROLIDINONE

• Additional metabolites isolated and identified by liquid chromatography-tandem mass spectrometry, and accounting for 1 to 5% of the excreted radioactivity in rat feces during the first 24 h, included two monohydroxylevormeloxifene species, a pyrrolidinone ring-opened metabolite of levormeloxifene, and desmethylnorlevormeloxifene [20].
• We here investigated the effects of nebracetam (WEB 1881 FU 4-aminomethyl-1-benzylpyrrolidin-2-one-hemifumarate), a novel pyrrolidinone nootropic, on the rise of intracellular Ca2+ concentration ([Ca2+]i) in Jurkat cells, a human leukemic T cell line [21].
• When the transport of PD was tested using the in situ brain perfusion technique, it was clarified that PD was not transported across the blood-brain barrier (BBB) by a neutral amino acid carrier system [22].

Associations of PYRROLIDINONE with other chemical compounds

• METHODS: In vivo measurements of GABA, homocarnosine, and pyrrolidinone were made of a 14-cc volume in the occipital cortex using 1H spectroscopy with a 2.1-Tesla magnetic resonance spectrometer and an 8-cm surface coil [23].
• In a double-blind, placebo-controlled, cross-over trial, the antihypoxidotic properties of BMS-181168 (previously BMY 21502)--a 1-[[1-[2-(trifluoromethyl)-4-pyrimidinyl]-4-piperidinyl]methyl]-2- pyrrolidinone alleviating impairment of learning and memory in the animal--were studied utilizing EEG mapping under an experimental hypoxic hypoxidosis [24].
• A long DNA molecule was used to guide the assembly of pyrrolidinone-capped Fe2O3 and CoFe2O3 particles as well as polylysine-coated gold nanoparticles [25].
• Three of five obtained analogues, pyrrolidinone, oxazolidinone and thiazolidinone demonstrated an interesting, specific odor which was compared with floral, typical jasmine odor of jasmone [26].

Gene context of PYRROLIDINONE

• A novel series of imidazolidinone-based matrix metalloproteinase (MMP) inhibitors was discovered by structural modification of pyrrolidinone la [27].
• Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold [28].

Analytical, diagnostic and therapeutic context of PYRROLIDINONE

• Pyrrolidinone was identified in food and tobacco samples by gas chromatography combined with NO-specific chemiluminescence detection (TEA) [15].
• The plasma concentration-time profiles of AP and its metabolites following oral administration of AP (50 and 100 mg/kg) were similar to those after iv dosing, with the exception of PD, which showed much lower plasma levels than those after iv administration [29].
• Determination of pyrrolidinone in plasma by high-performance liquid chromatography [30].

References