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Pesquisa : D03.633.100.221 [Categoria DeCS]
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  1 / 1955 MEDLINE  
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[PMID]:29268131
[Au] Autor:Duroux R; Agouridas L; Renault N; El Bakali J; Furman C; Melnyk P; Yous S
[Ad] Endereço:Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
[Ti] Título:Antagonists of the adenosine A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.
[So] Source:Eur J Med Chem;144:151-163, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:We have recently reported a series of 2-furoyl-benzoxazoles as potential A adenosine receptor (A R) antagonists. Two hits were identified with interesting pharmacokinetic properties but were find to bind the hA R receptor in the micromolar-range. Herein, in order to enhance affinity toward the hA R, we explored the C5- and C7-position of hits 1 and 2 based on docking studies. These modifications led to compounds with nanomolar-range affinity (e.g. 6a, Ki = 40 nM) and high antagonist activity (e.g. 6a, IC = 70.6 nM). Selected compounds also exhibited interesting in vitro DMPK (Drug Metabolism and Pharmacokinetics) properties including high solubility and low cytotoxicity. Therefore, the benzoxazole ring appears as a highly effective scaffold for the design of new A antagonists.
[Mh] Termos MeSH primário: Antagonistas do Receptor A2 de Adenosina/química
Antagonistas do Receptor A2 de Adenosina/farmacologia
Benzoxazóis/química
Benzoxazóis/farmacologia
Receptor A2A de Adenosina/metabolismo
[Mh] Termos MeSH secundário: Antagonistas do Receptor A2 de Adenosina/metabolismo
Antagonistas do Receptor A2 de Adenosina/farmacocinética
Benzoxazóis/metabolismo
Benzoxazóis/farmacocinética
Células CACO-2
Linhagem Celular Tumoral
Desenho de Drogas
Seres Humanos
Microssomos Hepáticos/metabolismo
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adenosine A2 Receptor Antagonists); 0 (Benzoxazoles); 0 (Receptor, Adenosine A2A)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


  2 / 1955 MEDLINE  
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[PMID]:29324338
[Au] Autor:Gamba E; Mori M; Kovalenko L; Giannini A; Sosic A; Saladini F; Fabris D; Mély Y; Gatto B; Botta M
[Ad] Endereço:Dipartimento di Scienze del Farmaco, Università di Padova, via Marzolo 5, 35131 Padova, Italy.
[Ti] Título:Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein.
[So] Source:Eur J Med Chem;145:154-164, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In this report, we present a new benzoxazole derivative endowed with inhibitory activity against the HIV-1 nucleocapsid protein (NC). NC is a 55-residue basic protein with nucleic acid chaperone properties, which has emerged as a novel and potential pharmacological target against HIV-1. In the pursuit of novel NC-inhibitor chemotypes, we performed virtual screening and in vitro biological evaluation of a large library of chemical entities. We found that compounds sharing a benzoxazolinone moiety displayed putative inhibitory properties, which we further investigated by considering a series of chemical analogues. This approach provided valuable information on the structure-activity relationships of these compounds and, in the process, demonstrated that their anti-NC activity could be finely tuned by the addition of specific substituents to the initial benzoxazolinone scaffold. This study represents the starting point for the possible development of a new class of antiretroviral agents targeting the HIV-1 NC protein.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/farmacologia
Benzoxazóis/farmacologia
HIV/efeitos dos fármacos
Proteínas do Nucleocapsídeo/antagonistas & inibidores
[Mh] Termos MeSH secundário: Fármacos Anti-HIV/síntese química
Fármacos Anti-HIV/química
Benzoxazóis/síntese química
Benzoxazóis/química
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Estrutura Molecular
Proteínas do Nucleocapsídeo/metabolismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Benzoxazoles); 0 (Nucleocapsid Proteins); 3X996Q809V (benzoxazolone)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE


  3 / 1955 MEDLINE  
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[PMID]:29310027
[Au] Autor:Malapati P; Krishna VS; Nallangi R; Srilakshmi RR; Sriram D
[Ad] Endereço:Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Jawaharnagar, RangaReddy District, Hyderabad 500 078, India.
[Ti] Título:Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
[So] Source:Eur J Med Chem;145:23-34, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In the present study, we attempted to develop novel class of Mycobacterium tuberculosis (Mtb) inhibitors by exploring the pharmaceutically underexploited enzyme targets which are majorly involved in cell wall biosynthesis of mycobacteria. For this purpose glutamate racemase was selected which racemizes d-glutamate from l-glutamate, a key step in peptidoglycan synthesis. Furthermore, enzyme is neither expressed nor its product, d-glutamate is produced in mammals, and hence inhibiting this enzyme will have no vulnerable effect in host organism. A library of our in-house compounds were screened against glutamate racemase using a biophysical technique; thermal shift assay and further by enzyme inhibition assay to identify Lead 1 molecule. Lead 1 optimization and expansion resulted in twenty four compounds. Among the synthesized compounds twelve compounds shown good enzyme inhibition than Lead 1 (IC 20.07 ±â€¯0.29 µM). Among all the compounds; compound 22 (IC 1.1 ±â€¯0.52 µM) showed potent non-competitive mode of inhibition in enzyme assay. Further showed good susceptibility (in replicating bacteria) of MIC 8.72 µM and bactericidal time dependant kill on dormant culture. It also exhibited significant activity in Mtb nutrient starvation model (2.5) and Mtb biofilm model (2.4) and in vivo M. marinum infected Zebra fish model studies (3.6) reduction at logarithmic scale.
[Mh] Termos MeSH primário: Isomerases de Aminoácido/antagonistas & inibidores
Antibacterianos/farmacologia
Benzoxazóis/farmacologia
Inibidores Enzimáticos/farmacologia
Mycobacterium/efeitos dos fármacos
[Mh] Termos MeSH secundário: Isomerases de Aminoácido/metabolismo
Animais
Antibacterianos/síntese química
Antibacterianos/química
Benzoxazóis/síntese química
Benzoxazóis/química
Biofilmes/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Cinética
Camundongos
Testes de Sensibilidade Microbiana
Simulação de Acoplamento Molecular
Estrutura Molecular
Mycobacterium/enzimologia
Células RAW 264.7
Relação Estrutura-Atividade
Peixe-Zebra
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Benzoxazoles); 0 (Enzyme Inhibitors); EC 5.1.1.- (Amino Acid Isomerases); EC 5.1.1.3 (glutamate racemase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180109
[St] Status:MEDLINE


  4 / 1955 MEDLINE  
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[PMID]:29232587
[Au] Autor:Tseng CH; Lin CK; Chen YL; Tseng CK; Lee JY; Lee JC
[Ad] Endereço:School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 807, Taiwan; Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 807, Taiwan; Research Center for Natural Products and Drug Development, Kaohsiung Medical
[Ti] Título:Discovery of naphtho[1,2-d]oxazole derivatives as potential anti-HCV agents through inducing heme oxygenase-1 expression.
[So] Source:Eur J Med Chem;143:970-982, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A number of naphtho[1,2-d]oxazole derivatives were synthesized and evaluated for their anti-HCV virus activity. Among them, compound 18 was the most active, exhibited approximately 21-folds more active anti-HCV activity (IC of 0.63 µM) than that of ribavirin (IC = 13.16 µM). Compound 18 was less cytotoxic than ribavirin, and the selective index (SI) of 18 is approximately 28-folds higher than that of ribavirin (229.10 v.s. 8.08). By using heme oxygenase-1 (HO-1) promoter-based assay and western blotting, compound 18 could induce HO-1 promoter activity, and protein expression. The antiviral effect of compound 18 was attenuated by HO-1 specific inhibitor SnPP treatment, which indicated that compound 18 suppressed HCV replication through inducing HO-1 expression. We further found that compound 18 reduced bach1 expression resulting in increasing the activity of Nrf-2 binding element. Moreover, the induction of HO-1 by compound 18 reduced HCV NS3/4A protease activity and induced the antiviral interferon responses. Therefore, compound 18 can be considered as a supplemental antiviral agent or a lead compound for further developing more effective agents against HCV replication.
[Mh] Termos MeSH primário: Compostos de Anilina/farmacologia
Antivirais/farmacologia
Benzoxazóis/farmacologia
Descoberta de Drogas
Heme Oxigenase-1/genética
Hepacivirus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Compostos de Anilina/síntese química
Compostos de Anilina/química
Antivirais/síntese química
Antivirais/química
Benzoxazóis/síntese química
Benzoxazóis/química
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Perfilação da Expressão Gênica
Seres Humanos
Estrutura Molecular
Reação em Cadeia da Polimerase em Tempo Real
Relação Estrutura-Atividade
Células Tumorais Cultivadas
Replicação Viral/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(furan-2-yl)-N-(4-methoxyphenyl)naphtho(1,2-d)oxazol-5-amine); 0 (Aniline Compounds); 0 (Antiviral Agents); 0 (Benzoxazoles); EC 1.14.14.18 (HMOX1 protein, human); EC 1.14.14.18 (Heme Oxygenase-1)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE


  5 / 1955 MEDLINE  
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[PMID]:27771284
[Au] Autor:Moorman DE; James MH; Kilroy EA; Aston-Jones G
[Ad] Endereço:Department of Neurosciences, Medical University of South Carolina, Charleston, SC 29425, USA; Department of Psychological and Brain Sciences & Neuroscience and Behavior Graduate Program, University of Massachusetts Amherst, Amherst, MA 01003, USA. Electronic address: moorman@cns.umass.edu.
[Ti] Título:Orexin/hypocretin-1 receptor antagonism reduces ethanol self-administration and reinstatement selectively in highly-motivated rats.
[So] Source:Brain Res;1654(Pt A):34-42, 2017 Jan 01.
[Is] ISSN:1872-6240
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The orexin/hypocretin (ORX) system regulates motivation for natural rewards and drugs of abuse such as alcohol. ORX receptor antagonists, most commonly OX1R antagonists including SB-334867 (SB), decrease alcohol drinking, self-administration and reinstatement in both genetically-bred alcohol-preferring and outbred strains of rats. Importantly, levels of alcohol seeking and drinking in outbred rats are variable, as they are in humans. We have shown that OX1R antagonism selectively decreases homecage alcohol drinking in high-, but not low-alcohol-preferring rats. It is unknown, however, whether this effect is selective to homecage drinking or whether it also applies to alcohol seeking paradigms such as self-administration and reinstatement following extinction, in which motivation is high in the absence of alcohol. Here we trained Sprague Dawley rats to self-administer 20% ethanol paired with a light-tone cue on an FR3 regimen. Rats were then extinguished and subjected to cue-induced reinstatement. Rats were segregated into high- and low-ethanol-responding groups (HR and LR) based on self-administration levels. During self-administration and cue-induced reinstatement, rats were given SB or vehicle prior to ethanol seeking. In both conditions, OX1R antagonism decreased responding selectively in HR, but not LR rats. There were no non-specific effects of SB treatment on arousal or general behavior. These data indicate that ORX signaling at the OX1R receptor specifically regulates high levels of motivation for alcohol, even in the absence of direct alcohol reinforcement. This implicates the ORX system in the pathological motivation underlying alcohol abuse and alcoholism and demonstrates that the OX1R may be an important target for treating alcohol abuse.
[Mh] Termos MeSH primário: Consumo de Bebidas Alcoólicas/tratamento farmacológico
Benzoxazóis/farmacologia
Depressores do Sistema Nervoso Central/administração & dosagem
Comportamento de Procura de Droga/efeitos dos fármacos
Etanol/administração & dosagem
Antagonistas dos Receptores de Orexina/farmacologia
Ureia/análogos & derivados
[Mh] Termos MeSH secundário: Consumo de Bebidas Alcoólicas/metabolismo
Transtornos Relacionados ao Uso de Álcool/tratamento farmacológico
Transtornos Relacionados ao Uso de Álcool/metabolismo
Animais
Animais não Endogâmicos
Condicionamento Operante/efeitos dos fármacos
Condicionamento Operante/fisiologia
Sinais (Psicologia)
Modelos Animais de Doenças
Comportamento de Procura de Droga/fisiologia
Masculino
Motivação/efeitos dos fármacos
Motivação/fisiologia
Receptores de Orexina/metabolismo
Ratos Sprague-Dawley
Autoadministração
Ureia/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea); 0 (Benzoxazoles); 0 (Central Nervous System Depressants); 0 (Hcrtr1 protein, rat); 0 (Orexin Receptor Antagonists); 0 (Orexin Receptors); 3K9958V90M (Ethanol); 8W8T17847W (Urea)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE


  6 / 1955 MEDLINE  
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[PMID]:29176834
[Au] Autor:Wieczorek A; Dulski K; Niedzwiecki S; Alfs D; Bialas P; Curceanu C; Czerwinski E; Danel A; Gajos A; Glowacz B; Gorgol M; Hiesmayr B; Jasinska B; Kacprzak K; Kaminska D; Kaplon L; Kochanowski A; Korcyl G; Kowalski P; Kozik T; Krzemien W; Kubicz E; Kucharek M; Mohammed M; Pawlik-Niedzwiecka M; Palka M; Raczynski L; Rudy Z; Rundel O; Sharma NG; Silarski M; Uchacz T; Wislicki W; Zgardzinska B; Zielinski M; Moskal P
[Ad] Endereço:Faculty of Physics, Astronomy and Applied Computer Science, Jagiellonian University, Kraków, Poland.
[Ti] Título:Novel scintillating material 2-(4-styrylphenyl)benzoxazole for the fully digital and MRI compatible J-PET tomograph based on plastic scintillators.
[So] Source:PLoS One;12(11):e0186728, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A novel plastic scintillator is developed for the application in the digital positron emission tomography (PET). The novelty of the concept lies in application of the 2-(4-styrylphenyl)benzoxazole as a wavelength shifter. The substance has not been used as scintillator dopant before. A dopant shifts the scintillation spectrum towards longer wavelengths making it more suitable for applications in scintillators of long strips geometry and light detection with digital silicon photomultipliers. These features open perspectives for the construction of the cost-effective and MRI-compatible PET scanner with the large field of view. In this article we present the synthesis method and characterize performance of the elaborated scintillator by determining its light emission spectrum, light emission efficiency, rising and decay time of the scintillation pulses and resulting timing resolution when applied in the positron emission tomography. The optimal concentration of the novel wavelength shifter was established by maximizing the light output and it was found to be 0.05 ‰ for cuboidal scintillator with dimensions of 14 mm x 14 mm x 20 mm.
[Mh] Termos MeSH primário: Benzoxazóis/química
Imagem por Ressonância Magnética
Tomografia por Emissão de Pósitrons
Contagem de Cintilação/instrumentação
Estirenos/química
Tomografia
[Mh] Termos MeSH secundário: Luz
Peso Molecular
Polimerização
Espectrometria de Fluorescência
Temperatura Ambiente
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoxazoles); 0 (Styrenes)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171219
[Lr] Data última revisão:
171219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0186728


  7 / 1955 MEDLINE  
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[PMID]:28465103
[Au] Autor:Pero JE; Rossi MA; Lehman HDGF; Kelly MJ; Mulhearn JJ; Wolkenberg SE; Cato MJ; Clements MK; Daley CJ; Filzen T; Finger EN; Gregan Y; Henze DA; Jovanovska A; Klein R; Kraus RL; Li Y; Liang A; Majercak JM; Panigel J; Urban MO; Wang J; Wang YH; Houghton AK; Layton ME
[Ad] Endereço:Department of Medicinal Chemistry, Merck & Co., Inc., West Point, PA 19486, USA. Electronic address: joseph.e.pero@gsk.com.
[Ti] Título:Benzoxazolinone aryl sulfonamides as potent, selective Na 1.7 inhibitors with in vivo efficacy in a preclinical pain model.
[So] Source:Bioorg Med Chem Lett;27(12):2683-2688, 2017 06 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Studies on human genetics have suggested that inhibitors of the Na 1.7 voltage-gated sodium channel hold considerable promise as therapies for the treatment of chronic pain syndromes. Herein, we report novel, peripherally-restricted benzoxazolinone aryl sulfonamides as potent Na 1.7 inhibitors with excellent selectivity against the Na 1.5 isoform, which is expressed in the heart muscle. Elaboration of initial lead compound 3d afforded exemplar 13, which featured attractive physicochemical properties, outstanding lipophilic ligand efficiency and pharmacological selectivity against Na 1.5 exceeding 1000-fold. Key structure-activity relationships associated with oral bioavailability were leveraged to discover compound 17, which exhibited a comparable potency/selectivity profile as well as full efficacy following oral administration in a preclinical model indicative of antinociceptive behavior.
[Mh] Termos MeSH primário: Analgésicos/farmacologia
Benzoxazóis/farmacologia
Canal de Sódio Disparado por Voltagem NAV1.7/metabolismo
Dor/tratamento farmacológico
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Administração Oral
Analgésicos/administração & dosagem
Analgésicos/química
Animais
Benzoxazóis/administração & dosagem
Benzoxazóis/química
Disponibilidade Biológica
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Formaldeído/administração & dosagem
Seres Humanos
Camundongos
Estrutura Molecular
Miócitos de Músculo Liso/efeitos dos fármacos
Miócitos de Músculo Liso/metabolismo
Dor/induzido quimicamente
Ratos
Relação Estrutura-Atividade
Sulfonamidas/administração & dosagem
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics); 0 (Benzoxazoles); 0 (NAV1.7 Voltage-Gated Sodium Channel); 0 (Sulfonamides); 1HG84L3525 (Formaldehyde)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


  8 / 1955 MEDLINE  
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[PMID]:28910447
[Au] Autor:Qiao SN; Zhou W; Liu LL; Zhang DQ; Zhong YM
[Ad] Endereço:Institutes of Brain Science, Fudan University, Shanghai, China.
[Ti] Título:Orexin-A Suppresses Signal Transmission to Dopaminergic Amacrine Cells From Outer and Inner Retinal Photoreceptors.
[So] Source:Invest Ophthalmol Vis Sci;58(11):4712-4721, 2017 Sep 01.
[Is] ISSN:1552-5783
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Purpose: The neuropeptides orexin-A and orexin-B are widely expressed in the vertebrate retina; however, their role in visual function is unclear. This study investigates whether and how orexins modulate signal transmission to dopaminergic amacrine cells (DACs) from both outer retinal photoreceptors (rods and cones) and inner retinal photoreceptors (melanopsin-expressing intrinsically photosensitive retinal ganglion cells [ipRGCs]). Methods: A whole-cell voltage-clamp technique was used to record light-induced responses from genetically labeled DACs in flat-mount mouse retinas. Rod and cone signaling to DACs was confirmed pharmacologically (in wild-type retinas), whereas retrograde melanopsin signaling to DACs was isolated either pharmacologically (in wild-type retinas) or by genetic deletion of rod and cone function (in transgenic mice). Results: Orexin-A attenuated rod/cone-mediated light responses in the majority of DACs and inhibited all DACs that exhibited melanopsin-based light responses, suggesting that exogenous orexin suppresses signal transmission from rods, cones, and ipRGCs to DACs. In addition, orexin receptor 1 antagonist SB334867 and orexin receptor 2 antagonist TCS OX229 enhanced melanopsin-based DAC responses, indicating that endogenous orexins inhibit signal transmission from ipRGCs to DACs. We further found that orexin-A inhibits melanopsin-based DAC responses via orexin receptors on DACs, whereas orexin-A may modulate signal transmission from rods and cones to DACs through activation of orexin receptors on DACs and their upstream neurons. Conclusions: Our results suggest that orexins could influence visual function via the dopaminergic system in the mammalian retina.
[Mh] Termos MeSH primário: Células Amácrinas/metabolismo
Dopamina/metabolismo
Orexinas/farmacologia
Células Fotorreceptoras de Vertebrados/metabolismo
Células Ganglionares da Retina/metabolismo
Opsinas de Bastonetes/metabolismo
Transdução de Sinais/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Benzoxazóis/farmacologia
Feminino
Isoquinolinas/farmacologia
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Antagonistas dos Receptores de Orexina/farmacologia
Técnicas de Patch-Clamp
Piridinas/farmacologia
Ureia/análogos & derivados
Ureia/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea); 0 (1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-((4-pyridinylmethyl)amino)-1-butanone); 0 (Benzoxazoles); 0 (Isoquinolines); 0 (Orexin Receptor Antagonists); 0 (Orexins); 0 (Pyridines); 0 (Rod Opsins); 0 (melanopsin); 8W8T17847W (Urea); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170915
[St] Status:MEDLINE
[do] DOI:10.1167/iovs.17-21835


  9 / 1955 MEDLINE  
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[PMID]:28891347
[Au] Autor:Gulçin I; Abbasova M; Taslimi P; Huyut Z; Safarova L; Sujayev A; Farzaliyev V; Beydemir S; Alwasel SH; Supuran CT
[Ad] Endereço:a Department of Chemistry, Faculty of Sciences , Ataturk University , Erzurum , Turkey.
[Ti] Título:Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors.
[So] Source:J Enzyme Inhib Med Chem;32(1):1174-1182, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Compounds containing nitrogen and sulfur atoms can be widely used in various fields such as industry, medicine, biotechnology and chemical technology. Therefore, the reactions of aminomethylation and alkoxymethylation of mercaptobenzothiazole, mercaptobenzoxazole and 2-aminothiazole were developed. Additionally, the alkoxymethyl derivatives of mercaptobenzoxazole and 2-aminothiazole were synthesized by a reaction with hemiformals, which are prepared by the reaction of alcohols and formaldehyde. In this study, the inhibitory effects of these molecules were investigated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes and carbonic anhydrase I, and II isoenzymes (hCA I and II). Both hCA isoenzymes were significantly inhibited by the recently synthesized molecules, with K values in the range of 58-157 nM for hCA I, and 81-215 nM for hCA II. Additionally, the K parameters of these molecules for BChE and AChE were calculated in the ranges 23-88 and 18-78 nM, respectively.
[Mh] Termos MeSH primário: Benzotiazóis/farmacologia
Benzoxazóis/farmacologia
Inibidores da Anidrase Carbônica/farmacologia
Inibidores da Colinesterase/farmacologia
Tiazóis/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Benzotiazóis/síntese química
Benzotiazóis/química
Benzoxazóis/síntese química
Benzoxazóis/química
Butirilcolinesterase/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Anidrases Carbônicas/metabolismo
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Relação Estrutura-Atividade
Tiazóis/síntese química
Tiazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Benzoxazoles); 0 (Carbonic Anhydrase Inhibitors); 0 (Cholinesterase Inhibitors); 0 (Thiazoles); 5K8WKN668K (2-aminothiazole); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); EC 4.2.1.1 (Carbonic Anhydrases); G5BW2593EP (benzothiazole)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170912
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1368019


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[PMID]:28834433
[Au] Autor:Wang J; Mu FR; Jiao WH; Huang J; Hong LL; Yang F; Xu Y; Wang SP; Sun F; Lin HW
[Ad] Endereço:School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University , Shenyang 110016, People's Republic of China.
[Ti] Título:Meroterpenoids with Protein Tyrosine Phosphatase 1B Inhibitory Activity from a Hyrtios sp. Marine Sponge.
[So] Source:J Nat Prod;80(9):2509-2514, 2017 Sep 22.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Three new meroterpenoids, hyrtiolacton A (1), nakijinol F (2), and nakijinol G (3), along with three known ones, nakijinol B (4), nakijinol E (5), and dactyloquinone A (6), were isolated and characterized from a Hyrtios sp. marine sponge collected from the South China Sea. The new structures were determined based on extensive analysis of HRESIMS and NMR data, and their absolute configurations were assigned by a combination of single-crystal X-ray diffraction and electronic circular dichroism analyses. Hyrtiolacton A (1) represents an unprecedented meroterpenoid featuring an unusual 2-pyrone attached to the sesquiterpene core, which is the first example of a pyrone-containing 4,9-friedodrimane-type sesquiterpene. These compounds were evaluated for their protein tyrosine phosphatase (PTP1B) inhibitory and cytotoxic activities. Nakijinol G (3) showed PTP1B inhibitory activity with an IC value of 4.8 µM but no cytotoxicity against four human cancer cell lines.
[Mh] Termos MeSH primário: Benzoxazóis/isolamento & purificação
Benzoxazóis/farmacologia
Dysidea/química
Poríferos/química
Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores
Pironas/química
Sesquiterpenos/isolamento & purificação
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Benzoxazóis/química
Linhagem Celular Tumoral
China
Seres Humanos
Estrutura Molecular
Proteína Tirosina Fosfatase não Receptora Tipo 1/química
Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo
Sesquiterpenos/química
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-pyrone); 0 (Benzoxazoles); 0 (Pyrones); 0 (Sesquiterpenes); 0 (hyrtiolacton A); 0 (nakijinol B); 0 (nakijinol F); 0 (nakijinol G); EC 3.1.3.48 (PTPN1 protein, human); EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170824
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00435



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