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[PMID]:28926764
[Au] Autor:Abdel-Rahman SA; El-Gohary NS; El-Bendary ER; El-Ashry SM; Shaaban MI
[Ad] Endereço:Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
[Ti] Título:Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of cyclopenta(hepta)[b]thiophene and fused cyclohepta[b]thiophene analogs.
[So] Source:Eur J Med Chem;140:200-211, 2017 Nov 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:New series of cyclopenta(hepta)[b]thiophene and fused cyclohepta[b]thiophene analogs were synthesized. The new analogs were assessed for antibacterial efficacy toward Escherichia coli ATCC 12435, Bacillus cereus UW 85 and Staphylococcus aureus. Compounds 5a, 6b and 12 showed eminent activity toward all selected bacterial strains compared to ampicillin. The antifungal efficacy of the same analogs was also examined toward Candida albicans and Aspergillus fumigatus 293, whereas 5a,b and 12 showed excellent efficacy toward both of the tested fungi. Moreover, 4b, 6a, 14a and 17 demonstrated interesting antifungal efficacy toward A. fumigatus. The same analogs were assessed for antiquorum-sensing efficacy toward Chromobacterium violacium ATCC 12472, whereas 5a, 12 and 15a demonstrated moderate activity. The new analogs were also esteemed for in vitro antitumor activity over HepG2, MCF-7 and HT-29 cancer cell lines. Results indicated that 6b and 10 are the most potent analogs against the three tested cell lines. In addition, 5a, 6a, 7 and 15a displayed interesting activity toward all tested cell lines. The active in vitro antitumor analogs were screened for in vivo antitumor activity over EAC in mice as well as in vitro cytotoxicity toward W138 human normal cell line. Results demonstrated that 6a,b and 10 have the highest in vivo activity, and that all tested compounds were found to be less cytotoxic than 5-FU toward W138 normal cell line. The DNA-binding affinity of the active antimicrobial and/or antitumor analogs was also assessed, whereas 4a, 5b, 10 and 15a exhibited the highest affinity. In silico studies affirmed that the inspected compounds are compatible with Lipinski's rule of five with expected good oral absorption.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antifúngicos/farmacologia
Antineoplásicos/farmacologia
Bactérias/efeitos dos fármacos
Fungos/efeitos dos fármacos
Tiofenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Antibacterianos/síntese química
Antibacterianos/química
Antifúngicos/síntese química
Antifúngicos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Cicloeptanos/síntese química
Cicloeptanos/química
Cicloeptanos/farmacologia
Ciclopentanos/síntese química
Ciclopentanos/química
Ciclopentanos/farmacologia
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Camundongos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Relação Estrutura-Atividade
Tiofenos/síntese química
Tiofenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Antineoplastic Agents); 0 (Cycloheptanes); 0 (Cyclopentanes); 0 (Thiophenes)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170920
[St] Status:MEDLINE


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[PMID]:28644559
[Au] Autor:Wang Z; Udmark J; Börjesson K; Rodrigues R; Roffey A; Abrahamsson M; Nielsen MB; Moth-Poulsen K
[Ad] Endereço:Department of Chemistry and Chemical Engineering, Chalmers University of Technology, Gothenburg, Sweden.
[Ti] Título:Evaluating Dihydroazulene/Vinylheptafulvene Photoswitches for Solar Energy Storage Applications.
[So] Source:ChemSusChem;10(15):3049-3055, 2017 Aug 10.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Efficient solar energy storage is a key challenge in striving toward a sustainable future. For this reason, molecules capable of solar energy storage and release through valence isomerization, for so-called molecular solar thermal energy storage (MOST), have been investigated. Energy storage by photoconversion of the dihydroazulene/vinylheptafulvene (DHA/VHF) photothermal couple has been evaluated. The robust nature of this system is determined through multiple energy storage and release cycles at elevated temperatures in three different solvents. In a nonpolar solvent such as toluene, the DHA/VHF system can be cycled more than 70 times with less than 0.01 % degradation per cycle. Moreover, the [Cu(CH CN) ]PF -catalyzed conversion of VHF into DHA was demonstrated in a flow reactor. The performance of the DHA/VHF couple was also evaluated in prototype photoconversion devices, both in the laboratory by using a flow chip under simulated sunlight and under outdoor conditions by using a parabolic mirror. Device experiments demonstrated a solar energy storage efficiency of up to 0.13 % in the chip device and up to 0.02 % in the parabolic collector. Avenues for future improvements and optimization of the system are also discussed.
[Mh] Termos MeSH primário: Azulenos/química
Cicloeptanos/química
Dispositivos Lab-On-A-Chip
Processos Fotoquímicos
Energia Solar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azulenes); 0 (Cycloheptanes); 0 (dihydroazulene)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171102
[Lr] Data última revisão:
171102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700679


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[PMID]:28383176
[Au] Autor:Peng G; McEwen AG; Olieric V; Schmitt C; Albrecht S; Cavarelli J; Tarnus C
[Ad] Endereço:Paul Scherrer Institut (SLS) WSLB, 5232, Villigen, Suisse, Switzerland.
[Ti] Título:Insight into the remarkable affinity and selectivity of the aminobenzosuberone scaffold for the M1 aminopeptidases family based on structure analysis.
[So] Source:Proteins;85(8):1413-1421, 2017 Aug.
[Is] ISSN:1097-0134
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Aminopeptidases are ubiquitous hydrolases that cleave the N-terminal residues of proteins and oligopeptides. They are broadly distributed throughout all kingdoms of life and have been implicated in a wide variety of physiological processes, including viral infection, parasite metabolism, protein processing, regulation of peptide hormones, and cancer cell proliferation. Members of the M1 family, also termed gluzincins, are defined by two highly conserved motifs in the catalytic domain: a zinc-binding motif, HEXXH-(X18)-E; and an exopeptidase motif, GXMEN. We report the high-resolution X-ray structures of E. coli aminopeptidase N (PepN) in complex with three aminobenzosuberone scaffolds that display various Ki values (50, 0.33, and 0.034 µM) and provide a compelling view of the outstanding selectivity of these chemical entities for the M1 aminopeptidases. This series of inhibitors interacts as transition state mimics with highly conserved residues of the catalytic machinery and substrate recognition sites. Structural comparisons and model-building studies allowed a deep interpretation of the SAR observed for bacterial, as well as mammalian enzymes. Proteins 2017; 85:1413-1421. © 2017 Wiley Periodicals, Inc.
[Mh] Termos MeSH primário: Aminopeptidases/antagonistas & inibidores
Anisóis/química
Proteínas de Bactérias/antagonistas & inibidores
Cicloeptanos/química
Escherichia coli/química
Inibidores de Proteases/química
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Aminopeptidases/química
Aminopeptidases/genética
Aminopeptidases/metabolismo
Proteínas de Bactérias/química
Proteínas de Bactérias/genética
Proteínas de Bactérias/metabolismo
Domínio Catalítico
Clonagem Molecular
Cristalografia por Raios X
Epóxido Hidrolases/química
Epóxido Hidrolases/genética
Epóxido Hidrolases/metabolismo
Escherichia coli/enzimologia
Escherichia coli/genética
Expressão Gênica
Seres Humanos
Cinética
Modelos Moleculares
Ligação Proteica
Conformação Proteica em alfa-Hélice
Conformação Proteica em Folha beta
Domínios e Motivos de Interação entre Proteínas
Proteínas Recombinantes/química
Proteínas Recombinantes/genética
Proteínas Recombinantes/metabolismo
Alinhamento de Sequência
Homologia Estrutural de Proteína
Especificidade por Substrato
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anisoles); 0 (Bacterial Proteins); 0 (Cycloheptanes); 0 (Protease Inhibitors); 0 (Recombinant Proteins); 0 (amino-benzosuberone); 148265-34-3 (pepN protein, Bacteria); EC 3.3.2.- (Epoxide Hydrolases); EC 3.3.2.- (leukotriene A4 hydrolase); EC 3.4.11.- (Aminopeptidases)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170825
[Lr] Data última revisão:
170825
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170407
[St] Status:MEDLINE
[do] DOI:10.1002/prot.25301


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[PMID]:27717044
[Au] Autor:De Vreese R; Galle L; Depetter Y; Franceus J; Desmet T; Van Hecke K; Benoy V; Van Den Bosch L; D'hooghe M
[Ad] Endereço:SynBioC Research Group, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, 9000, Ghent, Belgium.
[Ti] Título:Synthesis of Potent and Selective HDAC6 Inhibitors Bearing a Cyclohexane- or Cycloheptane-Annulated 1,5-Benzothiazepine Scaffold.
[So] Source:Chemistry;23(1):128-136, 2017 Jan 01.
[Is] ISSN:1521-3765
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Selective inhibitors of histone deacetylase 6 (HDAC6) are an emerging class of pharmaceuticals due to the involvement of HDAC6 in different pathways related to neurodegenerative diseases, cancer, and immunology. Herein, the synthesis of ten new benzohydroxamic acids, constructed by employing the tetrahydrobenzothiazepine core as a privileged pharmacophoric unit, is described. This is the first report on the synthesis and isolation of octahydrodibenzothiazepines and octahydro-6H-benzocycloheptathiazepines, which were then used to develop a new class of HDAC6 inhibitors. Evaluations of their HDAC-inhibiting activity resulted in the identification of cis-N-(4-hydroxycarbamoylbenzyl)-1,2,3,4,4a,5,11,11a-octahydrodibenzo[b,e][1,4]thiazepine-10,10-dioxide and cis-N-(4-hydroxycarbamoylbenzyl)-7-trifluoromethyl-1,2,3,4,4a,5,11,11a-octahydrodibenzo[b,e][1,4]thiazepine-10,10-dioxide as highly potent and selective HDAC6 inhibitors with activity in the low nanomolar range, which also show excellent selectivity on the enzymatic and cellular levels. Furthermore, four promising inhibitors were subjected to an Ames fluctuation assay, which revealed no mutagenic effects associated with these structures.
[Mh] Termos MeSH primário: Inibidores de Histona Desacetilases/síntese química
Histona Desacetilases/metabolismo
Tiazepinas/química
[Mh] Termos MeSH secundário: Sítios de Ligação
Cicloeptanos/química
Cicloexanos/química
Desacetilase 6 de Histona
Inibidores de Histona Desacetilases/química
Histona Desacetilases/química
Seres Humanos
Concentração Inibidora 50
Isomerismo
Simulação de Dinâmica Molecular
Tiazepinas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,5-benzothiazepine); 0 (Cycloheptanes); 0 (Cyclohexanes); 0 (Histone Deacetylase Inhibitors); 0 (Thiazepines); 48K5MKG32S (Cyclohexane); EC 3.5.1.98 (HDAC6 protein, human); EC 3.5.1.98 (Histone Deacetylase 6); EC 3.5.1.98 (Histone Deacetylases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161008
[St] Status:MEDLINE
[do] DOI:10.1002/chem.201604167


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[PMID]:27780725
[Au] Autor:Ferrari F; Cerlesi MC; Malfacini D; Asth L; Gavioli EC; Journigan BV; Kamakolanu UG; Meyer ME; Yasuda D; Polgar WE; Rizzi A; Guerrini R; Ruzza C; Zaveri NT; Calo G
[Ad] Endereço:Section of Pharmacology, Department of Medical Sciences, and National Institute of Neurosciences, University of Ferrara, Italy.
[Ti] Título:In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations.
[So] Source:Eur J Pharmacol;793:1-13, 2016 Dec 15.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Nociceptin/Orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP). In this study novel nonpeptide NOP ligands were characterized in vitro in receptor binding and [ S]GTPγS stimulated binding in membranes of cells expressing human NOP and classical opioid receptors, calcium mobilization assay in cells coexpressing the receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, the electrically stimulated mouse vas deferens and the mouse colon bioassays. The action of the AT compounds were compared with standard NOP agonists (N/OFQ and Ro 65-6570) and the NOP selective antagonist SB-612111. AT compounds displayed high NOP affinity and behaved as NOP agonists in all the functional assays consistently showing the following rank order of potency AT-127≥AT-090≥AT-035>AT-004= AT-001. AT compounds behaved as NOP full agonists in the calcium mobilization and mouse colon assays and as partial agonists in the [ S]GTPγS and BRET assays. Interestingly AT-090 and AT-127, contrary to standard nonpeptide agonists that display G protein biased agonism, behaved as an unbiased agonists. AT-090 and AT-127 displayed higher NOP selectivity than Ro 65-6570 at native mouse receptors. AT-090 and AT-127 might be useful pharmacological tools for investigating the therapeutic potential of NOP partial agonists.
[Mh] Termos MeSH primário: Cicloeptanos/farmacologia
Piperidinas/farmacologia
Receptores Opioides/agonistas
Proteínas Recombinantes/metabolismo
[Mh] Termos MeSH secundário: Animais
Células CHO
Colo/efeitos dos fármacos
Colo/metabolismo
Cricetinae
Cricetulus
Cicloeptanos/metabolismo
Células HEK293
Seres Humanos
Ligantes
Masculino
Camundongos
Piperidinas/metabolismo
Receptores Opioides/genética
Receptores Opioides/metabolismo
Proteínas Recombinantes/genética
Ducto Deferente/efeitos dos fármacos
Ducto Deferente/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cycloheptanes); 0 (Ligands); 0 (Piperidines); 0 (Receptors, Opioid); 0 (Recombinant Proteins); 0 (cis-1-methyl-7-((4-(2,6-dichlorophenyl)piperidin-1-yl)methyl)-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol); 0 (nociceptin receptor)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170816
[Lr] Data última revisão:
170816
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161106
[St] Status:MEDLINE


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[PMID]:27629493
[Au] Autor:Zavatti M; Guida M; Maraldi T; Beretti F; Bertoni L; La Sala GB; De Pol A
[Ad] Endereço:Department of Surgical, Medical, Dental and Morphological Sciences with Interest in Transplants, Oncology and Regenerative Medicine, University of Modena and Reggio Emilia, Modena, Italy. Electronic address: manuela.zavatti@unimore.it.
[Ti] Título:Estrogen receptor signaling in the ferutinin-induced osteoblastic differentiation of human amniotic fluid stem cells.
[So] Source:Life Sci;164:15-22, 2016 Nov 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: Ferutinin is a diaucane sesquiterpene with a high estrogenic activity. Since ferutinin is able to enhance osteoblastic differentiation of human amniotic fluid stem cells (hAFSCs), the aim of this study was to evaluate the role of the estrogen receptors α (ERα) and G-protein coupled receptor 30 (GPR30) in ferutinin-mediated osteoblastic differentiation. Moreover, it was investigated if MEK/ERK and PI3K/Akt signaling pathways are involved in ferutinin-induced effects. MAIN METHODS: hAFSCs were cultured in a standard medium or in an osteoblastic medium for 14 or 21days and ferutinin was added at 10 M. Immunofluorescence techniques and Western-blot 21analysis were used to study estrogen receptors and signaling pathways. KEY FINDINGS: In both undifferentiated and differentiated hAFSCs we identified ERα and GPR30 with a nuclear or cytoplasmatic localization, respectively. The presence of ferutinin in the osteoblastic medium leads to an increase in ERα expression. To dissect the role of estrogen receptors, MPP and G15 were used to selectively block ERα and GPR30, respectively. Notably, ferutinin enhanced osteoblastic differentiation in cells challenged with G15. Ferutinin was able to increase ERK and Akt phosphorylations with a different timing activation. These phosphorylations were antagonized by PD0325901, a MEK inhibitor, and wortmannin, a PI3K inhibitor. Both MPP and G15 inhibited the ferutinin-induced MEK/ERK and PI3K/Akt pathway activations. In the osteoblastic condition, PD0325901, but not wortmannin, reduced the expression of OPN and RUNX-2, whereas ferutinin abrogated the down-modulation triggered by PD0325901. SIGNIFICANCE: PI3K/Akt pathways seems to mediate the enhancement of hAFSCs osteoblastic differentiation triggered by ferutinin through ERα.
[Mh] Termos MeSH primário: Benzoatos/farmacologia
Diferenciação Celular/efeitos dos fármacos
Diferenciação Celular/fisiologia
Cicloeptanos/farmacologia
Receptor alfa de Estrogênio/metabolismo
Receptores Estrogênicos/metabolismo
Receptores Acoplados a Proteínas-G/metabolismo
Sesquiterpenos/farmacologia
Transdução de Sinais/fisiologia
Células-Tronco/citologia
[Mh] Termos MeSH secundário: Líquido Amniótico/citologia
Benzamidas/farmacologia
Compostos Bicíclicos com Pontes/farmacologia
Difenilamina/análogos & derivados
Difenilamina/farmacologia
Inibidores Enzimáticos/farmacologia
Receptor alfa de Estrogênio/genética
Regulação da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Sistema de Sinalização das MAP Quinases/fisiologia
Osteoblastos/citologia
Osteoblastos/efeitos dos fármacos
Fosfatidilinositol 3-Quinases/metabolismo
Fosforilação/efeitos dos fármacos
Células-Tronco/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzamides); 0 (Benzoates); 0 (Bridged Bicyclo Compounds); 0 (Cycloheptanes); 0 (Enzyme Inhibitors); 0 (Estrogen Receptor alpha); 0 (GPER protein, human); 0 (PD 0325901); 0 (Receptors, Estrogen); 0 (Receptors, G-Protein-Coupled); 0 (Sesquiterpenes); 41743-44-6 (4-oxy-6-(4-oxybezoyloxy)dauc-8,9-en); 9N3CBB0BIQ (Diphenylamine); EC 2.7.1.- (Phosphatidylinositol 3-Kinases)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170203
[Lr] Data última revisão:
170203
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160916
[St] Status:MEDLINE


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[PMID]:27556433
[Au] Autor:Puri A; Gupta R
[Ad] Endereço:Department of Chemistry, The IIS University, Jaipur 302020, India. ankita.puri@iisuniv.ac.in.
[Ti] Título:Effect of Mono- and Poly-CH/P Exchange(s) on the Aromaticity of the Tropylium Ion.
[So] Source:Molecules;21(8), 2016 Aug 20.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:In view of the fact that the phosphorus atom in its low co-ordination state (coordination numbers 1 and 2) has been termed as the carbon copy, there have been attempts to investigate, theoretically as well as experimentally, the effect of the exchange(s) of CH- moiety with phosphorus atom(s) (CH/P) on the structural and other aspects of the classical carbocyclic and heterocyclic systems. Tropylium ion is a well-known non-benzenoid aromatic system and has been studied extensively for its aromatic character. We have now investigated the effect of mono- and poly-CH/P exchange(s) on the aromaticity of the tropylium ion. For this purpose, the parameters based on the geometry and magnetic properties, namely bond equalization, aromatic stabilization energies (ASE), Nucleus-Independent Chemical Shift (NICS) values, (NICS(0), NICS(1), NICS(1)zz), proton nucleus magnetic resonance (¹H-NMR) chemical shifts, magnetic susceptibility exaltation and magnetic anisotropic values of mono-, di-, tri- and tetra-phosphatropylium ions have been determined at the Density Functional Theory (DFT) (B3LYP/6-31+G(d)) level. Geometry optimization reveals bond length equalization. ASEs range from -46.3 kcal/mol to -6.2 kcal/mol in mono- and diphospha-analogues which are planar. However, the ions having three and four phosphorus atoms lose planarity and their ASE values approach the values typical for non-aromatic structures. Of the three NICS values, the NICS(1)zz is consistently negative showing aromatic character of all the systems studied. It is also supported by the magnetic susceptibility exaltations and magnetic anisotropic values. Furthermore, ¹H-NMR chemical shifts also fall in the aromatic region. The conclusion that mono-, di-, tri- and tetra-phosphatropylium ions are aromatic in nature has been further corroborated by determining the energy gap between the Highest Occupied Molecular Orbital (HOMO) and Lowest Unoccupied Molecular Orbital (LUMO) (HOMO - LUMO gap), which falls in the range, ca. 3 × 10(-19)-9 × 10(-19) J. The systems having more than four phosphorus atoms are not able to sustain their monocyclic structure.
[Mh] Termos MeSH primário: Cicloeptanos/química
Fósforo/química
[Mh] Termos MeSH secundário: Íons
Fenômenos Magnéticos
Estrutura Molecular
Espectroscopia de Prótons por Ressonância Magnética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cycloheptanes); 0 (Ions); 0 (tropylium); 27YLU75U4W (Phosphorus)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170421
[Lr] Data última revisão:
170421
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160825
[St] Status:MEDLINE


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[PMID]:26871459
[Au] Autor:Yu J; Lee JM; Ryoo JJ
[Ad] Endereço:Department of Chemistry, Kyungpook National University, Daegu, Korea.
[Ti] Título:Chiral separation on various modified amino alcohol-derived HPLC chiral stationary phases.
[So] Source:Chirality;28(4):276-81, 2016 Apr.
[Is] ISSN:1520-636X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:3,5-Dinitrobenzoyl chloride was previously used for the preparation of (R)-phenylglycinol- and (S)-leucinol-derived chiral stationary phases. In this study, 3,5-bis(trifluoromethyl)benzoyl chloride, 2-furoyl chloride, 2-theonyl chloride, 10,11-dihydro-5H-dibenzo[b,f]azepine-5-carbonyl chloride, diphenylcarbamoyl chloride, and 1-adamantanecarbonyl chloride were used to prepare six new phenylglycinol-derived chiral stationary phases (CSPs) and five new leucinol-derived CSPs. Using these 11 CSPs, chiral separation of nine π-acidic amino acid derivatives and five π-basic compounds was performed, and the separation results were compared. An adamantyl-derived CSP showed good separation.
[Mh] Termos MeSH primário: Adamantano/química
Amino Álcoois/química
[Mh] Termos MeSH secundário: Adamantano/análogos & derivados
Compostos de Bifenilo/química
Cromatografia Líquida de Alta Pressão
Cicloeptanos/química
Etanolaminas/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-adamantanecarbonyl chloride); 0 (10,11-dihydro-5H-dibenzo(a,d)cycloheptene); 0 (Amino Alcohols); 0 (Biphenyl Compounds); 0 (Cycloheptanes); 0 (Ethanolamines); 0 (diphenylcarbamoyl chloride); 630DL2N96B (N-phenylethanolamine); PJY633525U (Adamantane)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160313
[Lr] Data última revisão:
160313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160213
[St] Status:MEDLINE
[do] DOI:10.1002/chir.22576


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[PMID]:26867504
[Au] Autor:Asth L; Ruzza C; Malfacini D; Medeiros I; Guerrini R; Zaveri NT; Gavioli EC; Calo' G
[Ad] Endereço:Department of Biophysics and Pharmacology, Federal University of Rio Grande do Norte, Natal, Brazil.
[Ti] Título:Beta-arrestin 2 rather than G protein efficacy determines the anxiolytic-versus antidepressant-like effects of nociceptin/orphanin FQ receptor ligands.
[So] Source:Neuropharmacology;105:434-442, 2016 Jun.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND PURPOSE: Nociceptin/orphanin FQ (N/OFQ) receptor (NOP) agonists produce anxiolytic-like effects in rodents while antagonists promote antidepressant-like effects. The aim of this study was to investigate the effect on anxiety and depression of NOP receptor partial agonists such as the peptides [F/G]N/OFQ(1-13)NH2 and UFP-113 and the non-peptide AT-090. EXPERIMENTAL APPROACH: In vitro AT-090, UFP-113, and [F/G]N/OFQ(1-13)NH2 were tested for their ability to promote NOP/G-protein and NOP/ß-arrestin 2 interaction, using a bioluminescence resonance energy transfer assay. In vivo, they were tested in mice in the elevated plus maze (EPM) and in the forced swim (FST) tests. NOP partial agonists effects were systematically compared to those of full agonists (N/OFQ and Ro 65-6570) and antagonists (UFP-101 and SB-612111). KEY RESULTS: In vitro, AT-090, UFP-113, and [F/G]N/OFQ(1-13)NH2 promoted NOP/G protein interaction, with maximal effects lower than those evoked by N/OFQ and Ro 65-6570. AT-090 behaved as a NOP partial agonist also in inducing ß-arrestin 2 recruitment, while UFP-113 and [F/G]N/OFQ(1-13)NH2 were inactive in this assay. In vivo, AT-090 induced anxiolytic-like effects in the EPM but was inactive in the FST. Opposite results were obtained with UFP-113 and [F/G]N/OFQ(1-13)NH2. CONCLUSIONS AND IMPLICATIONS: NOP ligands producing similar effects on NOP/G protein interaction (partial agonism) but showing different effects on ß-arrestin 2 recruitment (partial agonism vs antagonism) elicited different actions on anxiety and mood. These results suggest that the action of a NOP ligand on emotional states is better predicted based on its ß-arrestin 2 rather than G-protein efficacy.
[Mh] Termos MeSH primário: Ansiolíticos/farmacologia
Antidepressivos/farmacologia
Proteínas de Ligação ao GTP/metabolismo
Receptores Opioides/efeitos dos fármacos
beta-Arrestina 2/metabolismo
[Mh] Termos MeSH secundário: Animais
Cicloeptanos/farmacologia
Emoções/efeitos dos fármacos
Proteínas de Ligação ao GTP/agonistas
Células HEK293
Seres Humanos
Imidazóis/farmacologia
Ligantes
Camundongos
Piperidinas/farmacologia
Compostos de Espiro/farmacologia
Natação/psicologia
beta-Arrestina 2/agonistas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (8-acenaphthen-1-yl-1-phenyl-1,3,8-triazaspiro(4.5)decan-4-one); 0 (Anti-Anxiety Agents); 0 (Antidepressive Agents); 0 (Cycloheptanes); 0 (Imidazoles); 0 (Ligands); 0 (Piperidines); 0 (Receptors, Opioid); 0 (Spiro Compounds); 0 (beta-Arrestin 2); 0 (cis-1-methyl-7-((4-(2,6-dichlorophenyl)piperidin-1-yl)methyl)-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol); 0 (nociceptin receptor); EC 3.6.1.- (GTP-Binding Proteins)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170901
[Lr] Data última revisão:
170901
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160213
[St] Status:MEDLINE


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[PMID]:26804029
[Au] Autor:Arcuri L; Viaro R; Bido S; Longo F; Calcagno M; Fernagut PO; Zaveri NT; Calò G; Bezard E; Morari M
[Ad] Endereço:Department of Medical Sciences, Section of Pharmacology, University of Ferrara, via Fossato di Mortara 17-19, 44121 Ferrara, Italy; Neuroscience Center and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 17-19, 44121 Ferrara, Italy.
[Ti] Título:Genetic and pharmacological evidence that endogenous nociceptin/orphanin FQ contributes to dopamine cell loss in Parkinson's disease.
[So] Source:Neurobiol Dis;89:55-64, 2016 May.
[Is] ISSN:1095-953X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:To investigate whether the endogenous neuropeptide nociceptin/orphanin FQ (N/OFQ) contributes to the death of dopamine neurons in Parkinson's disease, we undertook a genetic and a pharmacological approach using NOP receptor knockout (NOP(-/-)) mice, and the selective and potent small molecule NOP receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111). Stereological unbiased methods were used to estimate the total number of dopamine neurons in the substantia nigra of i) NOP(-/-) mice acutely treated with the parkinsonian neurotoxin 1-methyl-4-phenyl-1,2,5,6-tetrahydropyridine (MPTP), ii) naïve mice subacutely treated with MPTP, alone or in combination with SB-612111, iii) rats injected with a recombinant adeno-associated viral (AAV) vector overexpressing human mutant p.A53T α-synuclein, treated with vehicle or SB-612111. NOP(-/-) mice showed a 50% greater amount of nigral dopamine neurons spared in response to acute MPTP compared to controls, which was associated with a milder motor impairment. SB-612111, given 4 days after MPTP treatment to mimic the clinical condition, prevented the loss of nigral dopamine neurons and striatal dopaminergic terminals caused by subacute MPTP. SB-612111, administered a week after the AAV injections in a clinically-driven protocol, also increased by 50% both the number of spared nigral dopamine neurons and striatal dopamine terminals, and prevented accompanying motor deficits induced by α-synuclein. We conclude that endogenous N/OFQ contributes to dopamine neuron loss in pathogenic and etiologic models of Parkinson's disease through NOP receptor-mediated mechanisms. NOP receptor antagonists might prove effective as disease-modifying agents in Parkinson's disease, through the rescue of degenerating nigral dopamine neurons and/or the protection of the healthy ones.
[Mh] Termos MeSH primário: Neurônios Dopaminérgicos/metabolismo
Neurônios Dopaminérgicos/patologia
Transtornos Parkinsonianos/metabolismo
Transtornos Parkinsonianos/patologia
Receptores Opioides/metabolismo
Substância Negra/metabolismo
Substância Negra/patologia
[Mh] Termos MeSH secundário: Animais
Cicloeptanos/administração & dosagem
Neurônios Dopaminérgicos/efeitos dos fármacos
Deleção de Genes
Locomoção/efeitos dos fármacos
Intoxicação por MPTP
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Knockout
Antagonistas de Entorpecentes/administração & dosagem
Transtornos Parkinsonianos/genética
Piperidinas/administração & dosagem
Ratos
Ratos Sprague-Dawley
Receptores Opioides/genética
Substância Negra/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cycloheptanes); 0 (Narcotic Antagonists); 0 (Piperidines); 0 (Receptors, Opioid); 0 (cis-1-methyl-7-((4-(2,6-dichlorophenyl)piperidin-1-yl)methyl)-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol); 0 (nociceptin receptor)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170825
[Lr] Data última revisão:
170825
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160126
[St] Status:MEDLINE



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