Relevant bibliographies by topics / Nitroindazole

Contents

  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'Nitroindazole'

Author: Grafiati
Published: 24 April 2022

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Consult the lists of relevant articles, books, theses, conference reports, and other scholarly sources on the topic 'Nitroindazole.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Journal articles on the topic "Nitroindazole"

1

Eddahmi, Mohammed, Nuno M. M. Moura, Latifa Bouissane, Ouafa Amiri, M. Amparo F. Faustino, José A. S. Cavaleiro, Ricardo F. Mendes, Filipe A. A. Paz, Maria G. P. M. S. Neves, and El Mostapha Rakib. "A Suitable Functionalization of Nitroindazoles with Triazolyl and Pyrazolyl Moieties via Cycloaddition Reactions." Molecules 25, no. 1 (December 28, 2019): 126. http://dx.doi.org/10.3390/molecules25010126.

Full text
Abstract:
The alkylation of a series of nitroindazole derivatives with 1,2-dibromoethane afforded the corresponding N-(2-bromoethyl)- and N-vinyl-nitro-1H-indazoles. The Cu(I)-catalysed azide- alkyne 1,3-dipolar cycloaddition was selected to substitute the nitroindazole core with 1,4-disubstituted triazole units after converting one of the N-(2-bromoethyl)nitroindazoles into the corresponding azide. The reactivity in 1,3-dipolar cycloaddition reactions with nitrile imines generated in situ from ethyl hydrazono-α-bromoglyoxylates was studied with nitroindazoles bearing a vinyl unit. The corresponding nitroindazole-pyrazoline derivatives were obtained in good to excellent yields.
APA, Harvard, Vancouver, ISO, and other styles
2

Ooms, Frédéric, Bernadette Norberg, Emre M. Isin, Neal Castagnoli, Cornelis J. Van der Schyf, and Johan Wouters. "7-Nitroindazole." Acta Crystallographica Section C Crystal Structure Communications 56, no. 10 (October 15, 2000): e474-e475. http://dx.doi.org/10.1107/s0108270100011975.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

IBÁÑEZ-ESCRIBANO, ALEXANDRA, JUAN JOSÉ NOGAL-RUIZ, ALICIA GÓMEZ-BARRIO, VICENTE J. ARÁN, and JOSÉ ANTONIO ESCARIO. "In vitro trichomonacidal activity and preliminary in silico chemometric studies of 5-nitroindazolin-3-one and 3-alkoxy-5-nitroindazole derivatives." Parasitology 143, no. 1 (November 4, 2015): 34–40. http://dx.doi.org/10.1017/s0031182015001419.

Full text
Abstract:
SUMMARYA selection of 1,2-disubstituted 5-nitroindazolin-3-ones (1–19) and 3-alkoxy-5-nitroindazoles substituted at positions 1 (20–24) or 2 (25–39) from our in-house compound library were screened in vitro against the most common curable sexually transmitted pathogen, Trichomonas vaginalis. A total of 41% of the studied molecules (16/39) achieved a significant activity of more than 85% growth inhibition at the highest concentration assayed (100 µg mL−1). Among these compounds, 3-alkoxy-5-nitroindazole derivatives 23, 24, 25 and 27 inhibited parasite growth by more than 50% at 10 µg mL−1. In addition, the first two compounds (23, 24) still showed remarkable activity at the lowest dose tested (1 µg mL−1), inhibiting parasite growth by nearly 40%. Their specific activity towards the parasite was corroborated by the determination of their non-specific cytotoxicity against mammalian cells. The four mentioned compounds exhibited non-cytotoxic profiles at all of the concentrations assayed, showing a fair antiparasitic selectivity index (SI > 7·5). In silico studies were performed to predict pharmacokinetic properties, toxicity and drug-score using Molinspiration and OSIRIS computational tools. The current in vitro results supported by the virtual screening suggest 2-substituted and, especially, 1-substituted 3-alkoxy-5-nitroindazoles as promising starting scaffolds for further development of novel chemical compounds with the main aim of promoting highly selective trichomonacidal lead-like drugs with adequate pharmacokinetic and toxicological profiles.
APA, Harvard, Vancouver, ISO, and other styles
4

Saunders, Fiona D., Martin Westphal, Perenlei Enkhbaatar, Jianpu Wang, Konrad Pazdrak, Yoshimitsu Nakano, Atsumori Hamahata, et al. "Molecular biological effects of selective neuronal nitric oxide synthase inhibition in ovine lung injury." American Journal of Physiology-Lung Cellular and Molecular Physiology 298, no. 3 (March 2010): L427—L436. http://dx.doi.org/10.1152/ajplung.00147.2009.

Full text
Abstract:
Neuronal nitric oxide synthase is critically involved in the pathogenesis of acute lung injury resulting from combined burn and smoke inhalation injury. We hypothesized that 7-nitroindazole, a selective neuronal nitric oxide synthase inhibitor, blocks central molecular mechanisms involved in the pathophysiology of this double-hit insult. Twenty-five adult ewes were surgically prepared and randomly allocated to 1) an uninjured, untreated sham group ( n = 7), 2) an injured control group with no treatment ( n = 7), 3) an injury group treated with 7-nitroindazole from 1-h postinjury to the remainder of the 24-h study period ( n = 7), or 4) a sham-operated group subjected only to 7-nitroindazole to judge the effects in health. The combination injury was associated with twofold increased activity of neuronal nitric oxide synthase and oxidative/nitrosative stress, as indicated by significant increases in plasma nitrate/nitrite concentrations, 3-nitrotyrosine (an indicator of peroxynitrite formation), and malondialdehyde lung tissue content. The presence of systemic inflammation was evidenced by twofold, sixfold, and threefold increases in poly(ADP-ribose) polymerase, IL-8, and myeloperoxidase lung tissue concentrations, respectively (each P < 0.05 vs. sham). These molecular changes were linked to tissue damage, airway obstruction, and pulmonary shunting with deteriorated gas exchange. 7-Nitroindazole blocked, or at least attenuated, all these pathological changes. Our findings suggest 1) that nitric oxide formation derived from increased neuronal nitric oxide synthase activity represents a pivotal reactive agent in the patho-physiology of combined burn and smoke inhalation injury and 2) that selective neuronal nitric oxide synthase inhibition represents a goal-directed approach to attenuate the degree of injury.
APA, Harvard, Vancouver, ISO, and other styles
5

Gutiérrez-Sánchez, Gaizka, Ignacio García-Alonso, Jorge Gutiérrez Sáenz de Santa María, Ana Alonso-Varona, and Borja Herrero de la Parte. "Antioxidant-Based Therapy Reduces Early-Stage Intestinal Ischemia-Reperfusion Injury in Rats." Antioxidants 10, no. 6 (May 27, 2021): 853. http://dx.doi.org/10.3390/antiox10060853.

Full text
Abstract:
Intestinal ischemia-reperfusion injury (i-IRI) is a rare disorder with a high mortality rate, resulting from the loss of blood flow to an intestinal segment. Most of the damage is triggered by the restoration of flow and the arrival of cytokines and reactive oxygen species (ROS), among others. Inactivation of these molecules before tissue reperfusion could reduce intestinal damage. The aim of this work was to analyze the preventive effect of allopurinol and nitroindazole on intestinal mucosal damage after i-IRI. Wag/RijHsd rats were subjected to i-IRI by clamping the superior mesenteric artery (for 1 or 2 h) followed by a 30 min period of reperfusion. Histopathological intestinal damage (HID) was assessed by microscopic examination of histological sections obtained from injured intestine. HID was increased by almost 20% by doubling the ischemia time (from 1 to 2 h). Nitroindazole reduced HID in both the 1 and 2 h period of ischemia by approximately 30% and 60%, respectively (p < 0.001). Our preliminary results demonstrate that nitroindazole has a preventive/protective effect against tissue damage in the early stages of i-IRI. However, to better understand the molecular mechanisms underlying this phenomenon, further studies are needed.
APA, Harvard, Vancouver, ISO, and other styles
6

Editorial, E. "Retraction: 7-nitroindazole, a selective neuronal nitric oxide synthase inhibitor in vivo prevents kainate-induced intrahippocampal neurotoxicity. Radenovic L, Selakovic V, Bozic B. Arch Biol Sci. 2005;57(2)75-81. DOI: 10.2298/ABS0502075R." Archives of Biological Sciences 68, no. 3 (2016): 691. http://dx.doi.org/10.2298/abs160412036e.

Full text
Abstract:
The article: 7-Nitroindazole, a selective neuronal nitric oxide synthase inhibitor in vivo prevents kainate-induced intrahippocampal neurotoxicity. Radenovic L, Selakovic V, Bozic B. Arch Biol Sci. 2005;57(2)75-81, repeats data already published in: 7-Nitroindazole reduces nitrite concentration in rat brain after intrahippocampal kainate-induced seizure. Radenovic L, Vasiljevic I, Selakovic V, Jovanovic M. Comp Biochem Physiol Pt. C. 2003;135 443-50, without any referencing. <br><br><font color="red"><b> Link to the retracted article <u><a href="http://dx.doi.org/10.2298/ABS0502075R">10.2298/ABS0502075R</a></b></u>
APA, Harvard, Vancouver, ISO, and other styles
7

Wiciński, M., G. Grześk, B. Malinowski, E. Grześk, A. T. Sinjab, M. Krzyżanowski, A. Michalska, et al. "Imidazole-induced contractility of vascular smooth muscle cells in the presence of U-73122, ODQ, indomethacin and 7-nitroindazole." Polish Journal of Veterinary Sciences 16, no. 2 (June 1, 2013): 293–97. http://dx.doi.org/10.2478/pjvs-2013-0040.

Full text
Abstract:
Abstract The aim of the study was to assess the impact of modulating factors on vascular smooth muscle cells reactivity. Vascular resistance was induced by the administration of increasing concentrations of imidazole. The experiments were performed on isolated and perfused tail artery of Wistar rats (weight 250 g - 350 g). Rats were been narcotized by urethane (intraperitoneal injection) at a dose of 120 mg/kg, stunned and then sacrificed by cervical dislocation. In the following investigation classical pharmacometric methods were used. Relationships between concentration-response curves (CRCs) for imidazole observed in the presence of ODQ [(1H-(1,2,4)oxadiazolo-[4,3-a]quinoxalin-1-one)], 7-nitroindazole and indomethacin were analyzed. Imidazole-induced contractility of vascular smooth muscle cells was independent from alpha- adrenergic receptors and PLC activity. Reactivity of VSMCsinduced by imidazole, was significantly changed in the presence of ODQ and 7-nitroindazole.
APA, Harvard, Vancouver, ISO, and other styles
8

Radenovic, Lidija, Vesna Selakovic, and Biljana Bozic. "7-nitroindazole, a selective neuronal nitric oxide synthase inhibitore in vivo, prevents kainate-induced intrahippocampal neurotoxicity." Archives of Biological Sciences 57, no. 2 (2005): 75–81. http://dx.doi.org/10.2298/abs0502075r.

Full text
Abstract:
We investigated the effects of 7-nitroindazole (7-NI), a selective neuronal nitric oxide synthase inhibitor in vivo, on nitrite concentration after kainic acid injection unilaterally into the CA3 region of the rat hippocampus. The accumulation of nitrite, the stable metabolite of NO, was measured by the Griess reaction at different times in hippocampus, forebrain cortex, striatum, and cerebellum homogenates. 7-nitroindazole can effectively inhibit NO synthesis in rat brain after kainate-induced neurotoxicity and suppressed nitrite accumulation. The present results suggest that neuronal NO synthase inhibitors may be useful in the treatment of neurological diseases in which excitotoxic mechanisms play a role. <br><br><font color="red"><b> This article has been retracted. Link to the retraction <u><a href="http://dx.doi.org/10.2298/ABS160412036E">10.2298/ABS160412036E</a><u></b></font>
APA, Harvard, Vancouver, ISO, and other styles
9

Jellestad, Finn Konow, and Hilde Gundersen. "Behavioral effects of 7-nitroindazole on hyperbaric oxygen toxicity." Physiology & Behavior 76, no. 4-5 (August 2002): 611–16. http://dx.doi.org/10.1016/s0031-9384(02)00765-5.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Aerschot, A. Van, J. Rozenski, D. Loakes, N. Pillet, G. Schepers, and P. Herdewijn. "An acyclic 5-nitroindazole nucleoside analogue as ambiguous nucleoside." Nucleic Acids Research 23, no. 21 (1995): 4363–70. http://dx.doi.org/10.1093/nar/23.21.4363.

Full text
APA, Harvard, Vancouver, ISO, and other styles
More sources

Dissertations / Theses on the topic "Nitroindazole"

1

Denadai, Magda Aline. "Efeitos do 7-nitroindazole, um inibidor da sintase neuronal do oxido nitrico (nNOS), sobre o condiciomaneto contextural em pombos." [s.n.], 2008. http://repositorio.unicamp.br/jspui/handle/REPOSIP/314745.

Full text
Abstract:
Orientador: Elenice Aparecida de Moraes Ferrari
Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia
Made available in DSpace on 2018-08-11T20:16:54Z (GMT). No. of bitstreams: 1 Denadai_MagdaAline_M.pdf: 823511 bytes, checksum: 1887972f9e5047fecbd7195247b586a8 (MD5) Previous issue date: 2008
Resumo: O óxido nítrico (NO), um neurotransmissor não convencional, tem papel importante em processos neurobiológicos de comportamento e de memória. Sua síntese é mediada por três isoformas de sintase do óxido nítrico (NOS): a neuronal (nNOS), a endotelial (eNOS) e induzível (iNOS). Este trabalho analisou o efeito do 7-nitroindazole (7-NI), um inibidor seletivo da nNOS, no condicionamento clássico aversivo em pombos. Foram usados 4 grupos: tratados com 7-NI (grupo 7-nitroindazole; G7-NI, n=5), tratados com óleo de amendoim (grupo veículo; GV, n=5), controle/sem tratamento (grupo controle; GC, n=5) e grupo não tratado/não condicionado (grupo manipulação; GM, n=5). A administração i.p. de 7-NI (25 mg/kg), ou do óleo de amendoim foi feita imediatamente após o treinamento. O G7-NI, o GV e o GC receberam três associações som-choque (5°, 10° e 15º minutos) numa sessão de 20 min. O teste a o contexto foi realizado 24 horas depois. As sessões foram gravadas para posterior transcrição e análise comportamental. A ocorrência da resposta de congelamento durante o treino não diferiu entre os grupos (p>0,05), mas durante o teste foi menor para o G7-NI em comparação ao treino (p<0.01) e aos demais grupos no teste (p<0.001). A atividade da NOS dependente de Ca++ no hipocampo foi menor no G7-NI do que nos outros grupos (p<0,01). Análise por Western blot indicou aumento na expressão de nNOS no G7-NI (p<0,05). A administração sistêmica de 7-NI teve um efeito amnésico sobre a memória contextual aversiva, indicando que a atividade da NOS dependente de Ca++ é importante para os processos de condicionamento clássico aversivo em pombos.
Abstract: Nitric oxide (NO) is an unsual neurotransmitter that plays an important role in neurobiological functions underlying behavior and memory. NO synthesis and release can be mediated by three isoforms of NO synthases (NOS): neuronal (nNOS), endothelial (eNOS) and inducible (iNOS). This study examined the effect of 7-nitroindazole (7-NI), a selective nNOS inhibitor, on contextual fear conditioning in pigeons. Four groups of pigeons were used: treated with 7-NI (7-NI; n=5), treated with peanut oil (Vehicle; n=5), non treated controls (Control; n=5) and non treated and no-trained controls (Non-trained; n=5). Treatment consisted in 7-NI (25 mg/kg; i.p.) or vehicle (peanut oil) administration, immediately after training. All the animals were trained in one 20 min session during which three tone-shock pairings (5th, 10th and 15th minutes) were presented. The test to the context was conducted 24h later. Behavioral categories were analyzed through the transcription of video-tapes of the sessions. The groups 7-NI, Vehicle and Control showed no significant differences in freezing during the conditioning session (p>0.05). During the test to the context the group 7-NI expressed significantly lower freezing as compared to Vehicle and Control (p<0.05). The 7-NI pigeons showed lower hippocampal activity of Ca++ dependent-NOS than Vehicle and Control groups (p<0.01). Western blot analysis indicated significant increase in nNOS expression (p<0.05). The systemic administration of 7-NI induced amnestic effects on contextual fear memory that evidence that Ca++-dependent NOS activity is required for fear conditioning in pigeons.
Mestrado
Fisiologia
Mestre em Biologia Funcional e Molecular
APA, Harvard, Vancouver, ISO, and other styles
2

Isin, Emre M. "Potential Prodrugs of the Neuronal Nitric Oxide Synthase and Monoamine Oxidase Inhibitor 7-Nitroindazole and Structurally Related Compounds." Thesis, Virginia Tech, 2000. http://hdl.handle.net/10919/35829.

Full text
Abstract:
Parkinson's disease (PD) is a progressive neurodegenerative disorder of unknown cause that afflicts about 1.5 million Americans. The characteristic feature of PD is a deficiency of dopamine in the terminals of nigrostriatal neurons. Two enzyme systems, the neuronal form of nitric oxide synthase (nNOS) and monoamine oxidase B (MAO-B), have been linked to neurodegenerative pathways leading to PD. Several MAO-B and nNOS inhibitors have been evaluated for their neuroprotective properties in the mouse model of neurodegeneration which employs the parkinsonian inducing neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). One such compound is 7-nitroindazole (7-NI), a compound which is reported to inhibit both enzymes.

This thesis focuses on the synthesis and biological evaluation of a potential prodrug form of 7-NI and related indazolyl containing compounds which are designed to release the active drugs following a metabolic bioactivation process. These studies have led to a detailed description of the nucleophilic aromatic substitution reactions between 4-chloro-1-methylpyridinium iodide and the indazolyl reactants that were employed as the initial step in the synthesis of the target compounds. The MAO-B substrate and inhibition properties of these "prodrugs" as well as the parent indazolyl compounds were examined. The results are discussed in relation to a previously developed active site model of MAO-B.
Master of Science

APA, Harvard, Vancouver, ISO, and other styles
3

Faria, Larissa Oliveira Melloni de 1985. "Participação da sintase neuronal de óxido nítrico (nNOS) na consolidação e reconsolidação da memória do condicionamento clássico aversivo em pombos (Columba livia)." [s.n.], 2013. http://repositorio.unicamp.br/jspui/handle/REPOSIP/314128.

Full text
Abstract:
Orientador: Elenice Aparecida de Moraes Ferrari
Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia
Made available in DSpace on 2018-08-23T06:24:39Z (GMT). No. of bitstreams: 1 Faria_LarissaOliveiraMellonide_M.pdf: 1121073 bytes, checksum: 5a3108ca0447b5fae98988b4611d7616 (MD5) Previous issue date: 2013
Resumo: O óxido nítrico (NO) é um neurotransmissor não convencional o qual tem papel importante em processos neurobiológicos de comportamento e de memória. Sua síntese é mediada por três isoformas de sintase do óxido nítrico (NOS): a neuronal (nNOS), a endotelial (eNOS) e a induzível (iNOS). Este trabalho investigou os efeitos da administração do 7- nitroindazol (7-NI), inibidor preferencial da nNOS, na consolidação e reconsolidação da memória do condicionamento clássico aversivo. Pombos adultos foram atribuídos a 5 grupos: Foram usados 5 grupos: grupo 7-nitroindazole (7-NI) (100nmol/0.5?/l; DMSO (20%), NaOH (50mM) e Tween-80 (16%) diluído em PBS; i.c.v.), grupo veículo (VEIC) (0,5?/l; DMSO (20%), NaOH (50mM) e Tween-80 (16%) diluído em PBS, i.c.v.), grupo condicionado/não tratado (COND), grupo contexto/não-tratado (CONT) e grupo não tratado/não condicionado (NÄIVE). Sete dias após implante de microcânula intracerebroventricular (i.c.v.), ocorreu o condicionamento com três associações contextochoque numa sessão de 20 min. O teste e o re-teste consistiram na re-exposição ao contexto do condicionamento por 5 min. O intervalo entre sessões foi de 24h. A administração de 7-NI ou do veículo ocorreu imediatamente após o treino (Experimento 1) ou após o re-teste (Experimento 2). A atividade enzimática da NOS dependente e independente de Ca2+ e da expressão protéica da nNOS foram realizadas no tecido hipocampal. No Experimento 1, a ocorrência de congelamento no teste do 7-NI foi menor do que no treino (p<0.01) e no teste do COND e VEIC (p < 0.001). A atividade da NOS dependente de Ca++ no 7-NI foi menor do que no COND e VEIC (p<0,01), mas não diferiu do CONT e do NÄIVE. A expressão protéica de nNOS não diferiu entre os grupos (p<0,05). No Experimento 2, houve diminuição dos comportamentos defensivos, incluindo o congelamento, no re-teste do 7-NI comparado com VEIC e COND (p<0.05), mas os grupos não diferiram quanto à atividade de NOS dependente de Ca2+ ou à expressão protéica da nNOS. Conclui-se que o 7-NI interferiu na consolidação e a reconsolidação da memória, indicando a ativação da via de sinalização do óxido nítrico no hipocampo em processos da memória de medo condicionado ao contexto em pombos
Abstract: Nitric oxide (NO) is an unconventional neurotransmitter which plays an important role in neurobiological processes of behavior and memory. Its synthesis is mediated by three isoforms of nitric oxide synthase (NOS): the neuronal (nNOS), the endothelial (eNOS) and the inducible (iNOS). This study investigated the effects of the administration of 7- nitroindazole (7-NI), a preferential nNOS inhibitor, in the consolidation and reconsolidation of aversive classical conditioning memory. Adult male pigeons were assigned to 5 groups: 7-nitroindazole, 7-NI (100nmol/0.5?/l; DMSO (20%), NaOH (50 mM) and Tween-80 (16%) diluted in PBS; i.c.v.) Vehicle group; VEH (0.5 ? / L; DMSO (20%), NaOH (50 mM) and Tween-80 (16%) diluted in PBS; i.c.v.), conditioning/non-treated group (COND), context/non-treated group (CONT) and non-conditioning/non-treated group (NÄIVE). Seven days after implantation of intracerebral ventricular (i.c.v.) microcannula the conditioning occurred with three context-shock associations in a session of 20 min. During the testing and retesting sessions pigeons were reexposed to the conditioning context for 5 min. The between sessions interval was 24h. Administration of 7-NI or vehicle occurred immediately after training (Experiment 1) or after testing (Experiment 2). The enzymatic activity of Ca2+ dependent and independent NOS and protein expression of nNOS in the hippocampus tissue were carried out following the behavioral test or retest. In Experiment 1, the occurrence of freezing in the testing session of 7-NI group was lower than in the training (p <0.01) and the testing sessions of COND and VEH groups (p <0.001). The activity of Ca2+ dependent NOS in the 7-NI group was lower than in COND and VEH groups (p <0.01) but did not differ from CONT and NÄIVE groups. The nNOS protein expression in the hippocampus did not differ among the different groups (p<0.05). In Experiment 2, there was a decrease of defensive behaviors, which include freezing, in the retest of the 7-NI compared with VEH and COND groups (p <0.05), but the groups did not differ in the activity of Ca2+ dependent NOS or the protein expression of nNOS. We conclude that 7-NI interfered on the consolidation and reconsolidation of memory, indicating activation of the nitric oxide signaling pathway in the hippocampus and in memory processes of conditioned fear context in pigeons
Mestrado
Fisiologia
Mestra em Biologia Funcional e Molecular
APA, Harvard, Vancouver, ISO, and other styles
4

McLoughlin, Claire Marie. "Effect of 7-nitroindazole and related indazoles on inducible nitric oxide synthase : implications for the treatment of septic shock." Thesis, King's College London (University of London), 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.271333.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Oosthuizen, Frasia. "The involvement of nitric oxide in a rodent model of post-traumatic stress disorder / Frasia Oosthuizen." Thesis, North-West University, 2003. http://hdl.handle.net/10394/418.

Full text
Abstract:
Post-traumatic stress disorder (PTSD), an anxiety disorder, may develop after experiencing or witnessing a severe traumatic event. Characteristic symptoms include hyper arousal and amnesic symptoms, while volume reductions in the hippocampus of these patients appear correlated with illness severity and the degree of cognitive deficit. Stress-induced increases in plasma cortisol have been implicated in this apparent atrophy of the hippocampus, although, clinical studies have described a marked suppression of plasma cortisol in PTSD. Given this hypocortisolemia, the basis for hippocampal neuro degeneration and cognitive decline remains unclear. While stress-related hippocampal structural changes have been linked to the neurotoxic effects of glucocorticoids and glutamate. NMDA-NO pathways have been found to play a causal role in anxiety-related behaviours. Prior exposure to trauma is an important risk factor for PTSD. In most instances the disorder becomes progressively worse over time, possibly with a delayed onset, suggesting a role for sensitization. In this study a time-dependent sensitization (TDS) model was used to induce PTSD-like sequelae in male Spraque-Dawley rats. The TDS-model is based on exposure to acute stressors, with a reminder of the trauma, in the form of re-exposure to one of the acute stressor, seven days later. NOS-activity, NMDA receptor parameters (Bmax and Kd) and GABA levels in the hippocampus of rats, as well as plasma corticosterone levels were determined 21 days after exposure to the TDS-model. Increased levels of corticosterone were measured after exposure to acute stress, but these levels were found to decrease below basal levels 21 days after the re-exposure, thus mimicking glucocorticoid levels in patients with PTSD. These findings may also imply that the increase in glucocorticoid levels after stress exposure is only the initial step in a cascade of events leading to neuronal damage in the hippocampus. This study also found that stress-restress evoked a long-lasting increase in hippocampal NOS activity that was accompanied by a reactive down-regulation of hippocampal NMDA receptors and dysregulation of inhibitory GABA pathways. Subsequently, animals were chronically treated with certain pharmacological agents prior to exposure to the TDS-model to determine possible approaches for inhibiting the induction of PTSD. Pre-treatment with fluoxetine, currently indicated in the treatment of PTSD. and the nNOS inhibitor, 7-nitroindazole, had no effect on the increased NOS activity measured 21 days afler exposure to the TDS-model. Pre-treatment with the iNOS inhibitor, aminoguanidine, however, resulted in inhibition of the observed increase in hippocampal NOS-activity, implicating a possible role for the iNOS isoform in the etiology of PTSD. Treatment with ketoconazole, an inhibitor of glucoccfticoid synthesis, resulted in inhibition of the increase in NOS-activity observed after exposure to TDS-stress, thus indicating a possible link between stress glucocorticoid-release and NO synthesis. These perturbations may have importance in explaining the increasing evidence for stress-related hippocampal degenerative pathology and cognitive deficits seen in patients with PTSD. Uncovering and understanding the role of NO in PTSD will hopefully lead to the development of selective therapeutic agents in disorders like PTSD. as well as providing a better understanding of basic processes underlying normal and pathological neuronal functions in PTSD.
Thesis (Ph.D. (Pharmacology))--North-West University, Potchefstroom Campus, 2004.
APA, Harvard, Vancouver, ISO, and other styles
6

Bothma, Tanya. "Investigating the role of the NO-cGMP pathway in an animal model of posttraumatic stress disorder (PTSD) / Tanya Bothma." Thesis, North-West University, 2004. http://hdl.handle.net/10394/477.

Full text
Abstract:
Posttraumatic stress disorder (PTSD) is a severe anxiety disorder characterised by hypothalamic-pituitary-adrenal (HPA)-axis abnormalities, hyperarousal, anxiety, flashbacks of trauma memories and avoidance. Increasing evidence is now accumulating that the disorder is also associated with shrinkage of the hippocampus and cognitive dysfunction that may have its origin in stress-induced excitotoxicity. Animal studies have indeed highlighted a potential role of the excitotoxic glutamatenitric oxide (NO) pathway in the stress response. Since PTSD appears to be an illness that progresses and worsens over time after an initial severe traumatic event, this study has used an animal model that emphasises repeated trauma to investigate the effect of stress on hippocampal NO synthase (NOS) activity, the release of the nitrogen oxide metabolites of NO (NOx), and also the evoked release of cGMP. Furthermore, the modulation and dependency of these responses on glutamate, NO and cGMP activity using drugs selective for these targets, will also be investigated. Rats (n=10/group) were exposed to repeated stress together with saline or drug administration immediately after the stress procedure and continuing for one week post-stress. The animals were then sacrificed for assay of hippocampal NOS activity, NO, and cGMP accumulation. Animals received either the glutamate-NMDA receptor antagonist, memantine (MEM;5mg/kg ip/d), the neuronal NOS selective inhibitor, 7- nitroindazole monosodium salt (7-NINA;20mg/kg ip/d), the cGMP-specific PDE inhibitor, sildenafil (SIL;10mg/kg ip/d) or the NFkb antagonist, pyrollidine dithiocarbamate (PDTC;70mg/kg ip/d). The latter inhibits the nuclear transcription factor, NFkb, responsible for inducing the expression of iNOS, while it also appears to mediate the glutamatergic actions on NOS expression, Stress significantly increased hippocampal NOS activity, as well as significantly increased hippocampal cGMP and NO, levels. These increases were blocked by pretreatment with either PDTC or 7-NINA, while memantine was without effect. Sildenafil significantly augmented stress induced NO, accumulation, as well as cGMP. although the latter failed to reach significance. 7-NINA and memantine significantly blocked the increase in cGMP evoked by time-dependent sensitisation (TDS)-stress, with PDTC attenuating this response, but not significantly. Additionally, administration of each drug separately for seven days without exposure to stress, did not evoke significant changes in NOx levels, compared to the control group. However, significant increases in cGMP levels, compared to the control group, were found with all four drugs. Repeated trauma therefore activates the NO-cGMP pathway, possibly involving actions on both nNOS and iNOS. The NMDA receptor appears less involved after chronic repeated stress, and may have limited therapeutic implications. Sub-cellular NO-modulation, however, may represent an important therapeutic strategy in preventing the effects of severe stress and in treating PTSD.
Thesis (M.Sc. (Pharmacology))--North-West University, Potchefstroom Campus, 2005.
APA, Harvard, Vancouver, ISO, and other styles
7

Harb, Hisham Labib. "Biochemical and pharmacological evaluation of the role of xanthine oxidase in the catabolism of 7-nitroindazole (7-ni) in the isolated rat mesentery in vitro and in the intact rat and mouse cardiovascular and antinociceptive effects." Thesis, King's College London (University of London), 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.268471.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Paucard, Alexia. "Etude des mécanismes mis en jeu lors d'un stress oxydatif induit par l'injection intrastriatale de malonate chez le rat." Paris 5, 2003. http://www.theses.fr/2003PA05P643.

Full text
Abstract:
L'existence d'un stress oxydatif (SO) a été rapportée dans diverses pathologies cérébrales. Dans ce contexte, notre travail a consisté à rechercher les mécanismes déclenchés par le SO ainsi que leur contribution à la mort neuronale. Le SO a été induit par l'injection de malonate (3 æmol), une toxine mitochondriale, dans le striatum de rats. Dans ce modèle, nous avons montré une chute précoce du glutathion total, le principal antioxydant endogène, associée à une lésion massive et à un œdème cérébral. L'a-phényl tert-butyl nitrone, un composé antioxydant, a exercé dans ce modèle un effet antiœdémateux. L'injection de malonate entraîne également une production de NO, par la NO-synthase neuronale. Ce NO module l'activation de la caspase 3, une des enzymes mises en jeu lors de la mort par apoptose. Cependant, l'inhibition de la caspase-3 n'a pas exercé d'effet neuroprotecteur. Le SO induit par le malonate déclenche donc des mécanismes conduisant principalement à une mort de type nécrotique
Oxidative stress (OS) has been reported in various cerebral pathogenesis. In this context, our work aimed to elucidate the mechanisms triggered by OS and their contribution to neuronal death. Our model of OS consisted in an injection of malonate (3 æmol), a mitochondrial toxin, in the striatum of rats. In this model, we showed an early drop of total glutathione, the major endogenous antioxidant, associated with a massive lesion and a cerebral edema. A-phenyl tert-butyl nitrone, an antioxidant compound, exerts in this model an antiedematous effect. Malonate injection was followed by NO production by the neuronal NO-synthase. This NO modulates caspase-3 activation, one of the enzymes implicated in apoptotic cell death. Nevertheless, inhibition of caspase-3 did not exert a neuroprotective effect. Thus the OS induced by malonate leads to neuronal death mainly through necrotic mechanisms
APA, Harvard, Vancouver, ISO, and other styles
9

Morales, Montecinos Javier Octavio. "Estudio Espectroscópico de la Inclusión de 5-Nitroindazol en Ciclodextrinas." Tesis, Universidad de Chile, 2007. http://repositorio.uchile.cl/handle/2250/105630.

Full text
Abstract:
Memoria para optar al título de Químico Farmacéutico
En esta tesis se estudió el efecto que tendrían la βCD y la 2,6-DMβCD sobre la solubilidad de un nuevo nitroderivado antichagásico, el 1-(2-(dimetilamino)etil)-3-metoxi-5- nitro-1H-indazol. Además se propuso la estructura tridimensional que adopta el 5-nitroindazol al interior de la cavidad de las diferentes CDs. Por medio de la metodología de variación continua y de solubilidad de fase, se encontró que ambas CDs generan compuestos de inclusión con una estequiometría de 1:1. Las constantes de asociación, Ka, encontradas fueron 186,5 M-1 y 3687,8 M-1 para la βCD y la DMβCD respectivamente. Se observó que 10 mM de βCD aumenta al doble la solubilidad del 5- NI; mientras que la DMβCD, a la misma concentración, aumenta seis veces la solubilidad del compuesto. El espectro ROESY del 5-NI libre permitió determinar la geometría que adopta el compuesto en solución acuosa. Se observó que el protón 7 del anillo aromático establece una interacción con los protones de la cadena alifática lateral, 1’, 2’ y 4’. Esto significaría que en solución, la cadena se encuentra plegada orientándose hacia la región aromática. Estos espectros también permiten establecer cómo es la inclusión del 5-NI al interior de las CDs. En el caso del complejo entre el 5-NI y βCD, el espectro ROESY indica que existen interacciones entre los protones aromáticos, 4, 6 y 7 del 5-NI y los protones del interior de la cavidad de la CD. Junto con esto se encontró que los protones que forman parte de la cadena alifática, 2’ y 4’, se desplazan cuando se encuentran formando el complejo de inclusión, lo que significaría que también interactúan con el interior de la cavidad. Lo anterior sugiere que el compuesto se incluye en la cavidad de la CD casi completamente. Por otro lado, también se observan interacciones entre el protón 7 del anillo aromático del 5-NI y los protones de la cadena alifática, indicando que ésta se encuentra plegada hacia la región aromática, de la misma forma que el 5-NI libre en solución. El complejo entre el 5-NI y la DMβCD, presenta una geometría de inclusión distinta, ya que las interacciones de la región aromática del 5-NI y los protones de la cavidad de la CD, indican que la orientación del 5-NI deja el núcleo bencénico hacia la abertura más ancha, mientras que el núcleo pirazólico, del indazol, hacia la abertura de diámetro menor. Además los desplazamientos de las señales de los protones de la cadena alifática, indican que se encuentra completamente incluida en la CD; sin embargo, se puede decir que la cadena se encuentra menos plegada en este complejo, pues no se observan interacciones con el protón 7 del 5-NI
In this thesis we studied the impact of the βCD and 2,6-DMβCD on the solubility of a new antichagasic nitroderivative, 1-(2-(dimethylamino) ethyl) -3-metoxi-5-nitro-1H-indazol . In addition, we proposed the three-dimensional structure that adopts 5-nitroindazol inside the cavity of different CDs. With the continuous variation and phase solubility methodologies, we found that both generate inclusion complexes with the different CDs. The stoichiometry was 1:1, and the asosiation constants, Ka, was 186.5 M-1 and 3687.8 M-1, for both βCD and DMβCD respectively. The geometry of the 5-NI derivative in aqueous solution, was determined by 2DROESY spectra. The aliphatic amino chain is folded and interacts with the aromatic H-7. The 2D-ROESY spectrum of the complex of 5-NI inside the CD, indicates that there are interactions between the aromatic protons, 4, 6 and 7 of 5-NI and protons inside the cavity of the CD. Besides the protons that are part of the aliphatic chain, 2' and 4’, they shift to a high filed when they are forming the inclusion complex. This suggests, that the compound is included in the cavity of the CD almost completely. On the other hand, there are certain interactions between the proton 7 of the aromatic ring of 5-NI and protons in the aliphatic chain, indicating that it is folded toward the aromatic region in the same way that 5-NI free solution . Whereas the complex between 5-NI and DMβCD, shows a different geometry of inclusion. Interactions of aromatic protons of the 5-NI with the CD, show that the orientation of 5-NI includes benzenic core towards the secondary rim, while the pirazolic core, is near the primary rim.
APA, Harvard, Vancouver, ISO, and other styles
10

Sánchez, Núñez Paulina Alejandra. "Estudio de reactividad y caracterización electroquímica de nitroindazoles con potencial actividad antichagásica." Tesis, Universidad de Chile, 2008. http://www.repositorio.uchile.cl/handle/2250/112021.

Full text
Abstract:
Memoria para optar al título de Químico
Este estudio fue desarrollado para investigar los mecanismos de reducción y reactividad de compuestos derivados de 5-nitroindazol, los cuales podrían tener actividad antitripanocida a través de un análisis de capacidad antioxidante por medio de la técnica de fluorescencia ORAC-FL y un estudio cinético UV-Vis, además de un estudio electroquímico. La formación del anión radical nitro fue estudiada por medio de voltametría cíclica, a través del cual se propuso un mecanismo de reducción común para todos los compuestos en estudio; una reducción monoelectrónica, seguido de una reacción ácido base y finalmente una segunda reducción monoelectrónica. Este mecanismo es debido a que estos compuestos poseen un hidrógeno lábil en sus estructuras. Para determinar la reactividad del hidrógeno lábil presente, se realizó un estudio de la capacidad antioxidante, a través del estudio ORAC-FL el cual determinó que el hidrogeno lábil presente en las estructuras de los compuestos estudiados es donado al radical libre AAPH en razón 1:1, por lo tanto se comprueba la labilidad de este hidrógeno. Por otra parte, se realizó el estudio de reactividad a través de la determinación de las constantes cinéticas de reacción por medio de la espectroscopia UV-Vis. En este estudio se pudo ver que la reacción de donación del hidrogeno lábil de los compuestos estudiados al radical DPPH es lenta, ya que se mostraron valores bajos de constantes de velocidad.
This study was undertaken to investigate the reduction mechanism and the reactivity of nitroindazole derivates, wich have antitrypanosida activity through a free radical-scavenging analysis by ORAC-FL assay and an UV-Vis kinetic study, moreover an electrochemical study. The nitro radical´s species formation was studied by cyclic voltametric, through which a common reduction mechanism was proposed; a monoelectronic reduction, followed by an acid-base equilibrium and finally a second monoelectronic reduction. The mechanism by which these compounds possess labile hydrogen in it structures. The antioxidant capacity of these compounds was determinate by the oxygen radical absorbing capacity assay using fluorescein (ORAC-FL), it showed that the labile proton present in this structures is given to the free radical AAPH in rate 1:1 therefore it is found the lability of this hydrogen. On the other hand, the reactivity of the nitroindazole derivates was studied through a kinetic study, by this assay were obtained the rate constants of the reduction reaction of DPPH radical for the antioxidant, it were obtained under pseudo-first-order conditions, lo which is studied by UV-Vis. The experimental results showed that the labile donation reaction of the hydrogen of the compounds studied the DPPH radical are slow, as it showed low rate constants.
APA, Harvard, Vancouver, ISO, and other styles
More sources

Book chapters on the topic "Nitroindazole"

1

Pardasani, R. T., and P. Pardasani. "Molar magnetic moment of iron(III)-nickel(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 2, 257–58. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62466-1_111.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Pardasani, R. T., and P. Pardasani. "Molar magnetic moment of cobalt(II)-nickel(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 2, 977–79. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62466-1_439.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Pardasani, R. T., and P. Pardasani. "Molar magnetic moment of iron(III)-copper(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 2, 259–60. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62466-1_112.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Pardasani, R. T., and P. Pardasani. "Molar magnetic moment of manganese(II)-copper(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 1, 853–54. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62478-4_348.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Pardasani, R. T., and P. Pardasani. "Molar magnetic moment of manganese(II)-nickel(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 1, 851–52. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62478-4_347.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Pardasani, R. T., and P. Pardasani. "Magnetic properties of hetero-binuclear nickel(II)-copper(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 3, 666–67. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62470-8_292.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Pardasani, R. T., and P. Pardasani. "Magnetic properties of hetero-binuclear copper(II)-nickel(II) complex with 5-nitroindazole and ethylenediamine." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 4, 1308–9. Berlin, Heidelberg: Springer Berlin Heidelberg, 2021. http://dx.doi.org/10.1007/978-3-662-62474-6_551.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Matteo, Vincenzo, Massimo Pierucci, Arcangelo Benigno, Gergely Orbán, Giuseppe Crescimanno, Ennio Esposito, and Giuseppe Giovanni. "Electrophysiological and Neurochemical Characterization of 7-Nitroindazole and Molsidomine Acute and Sub-Chronic Administration Effects in the Dopaminergic Nigrostrial System in Rats." In Birth, Life and Death of Dopaminergic Neurons in the Substantia Nigra, 173–82. Vienna: Springer Vienna, 2009. http://dx.doi.org/10.1007/978-3-211-92660-4_14.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Enna, S. J., and David B. Bylund. "7-Nitroindazole." In xPharm: The Comprehensive Pharmacology Reference, 1. Elsevier, 2007. http://dx.doi.org/10.1016/b978-008055232-3.63518-4.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Moore, Philip K., and Philip A. Bland-Ward. "7-Nitroindazole: An inhibitor of nitric oxide synthase." In Methods in Enzymology, 393–98. Elsevier, 1996. http://dx.doi.org/10.1016/s0076-6879(96)68041-0.

Full text
APA, Harvard, Vancouver, ISO, and other styles

Conference papers on the topic "Nitroindazole"

1

Cheptea, Corina, Andreea-Celia Benchea, Marius Gaina, Catalina Iulia Saveanu, Madalina Postaru, Dana Ortansa Dorohoi, Valeriu Sunel, and Marin Zagnat. "Synthesis and toxicological activity of 5-nitroindazole sulfonamides derivatives as potential antimicrobial agents. Optimization of the synthesis." In 2017 E-Health and Bioengineering Conference (EHB). IEEE, 2017. http://dx.doi.org/10.1109/ehb.2017.7995458.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Klinnikova, A. A., G. A. Danilova, and N. P. Aleksandrova. "The role of neuronal NO synthase in the respiratory effects of TNF-α." In VIII Vserossijskaja konferencija s mezhdunarodnym uchastiem «Mediko-fiziologicheskie problemy jekologii cheloveka». Publishing center of Ulyanovsk State University, 2021. http://dx.doi.org/10.34014/mpphe.2021-115-118.

Full text
Abstract:
It was shown that an increase level of proinflammatory cytokines has a modulating effect on the reflex control of respiration. The aim of this study was to investigate the involvement of neuronal nitric oxide synthase (nNOS) in the mechanisms of the influence of an increased level of Tumor necrosis factor – α (TNF-α) on the hypoxic ventilatory response. To achieve this goal, experiments were carried out on urethane anesthetized rats with intravenous administration of TNF-α before and after pretreatment with 7-nitroindazole specific nNOS inhibitor. The hypoxic ventilation response was assessed by rebreathing with a hypoxic gas mixture before and after administration of TNF-α. We found that TNF-α decreased the ventilatory response to hypoxia. Pretreatment with nNOS inhibitor reduced respiratory effects of TNF-α. Key words: cytokines, TNF-α, hypoxia, chemoreflex, respiration, ventilation, neuronal nitric oxide synthase.
APA, Harvard, Vancouver, ISO, and other styles
3

Seela, Frank, and Anup M. Jawalekar. "4-Nitroindazole: Its ambiguous nature in oligonucleotide base pairing and the influence of the glycosylation position on the duplex stability." In XIIth Symposium on Chemistry of Nucleic Acid Components. Prague: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 2002. http://dx.doi.org/10.1135/css200205338.

Full text
APA, Harvard, Vancouver, ISO, and other styles
You might also be interested in the extended bibliographies on the topic 'Nitroindazole' for particular source types:
Journal articles Dissertations / Theses
We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!

To the bibliography