Base de dados : MEDLINE
Pesquisa : D02.491 [Categoria DeCS]
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  1 / 4707 MEDLINE  
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[PMID]:29184947
[Au] Autor:Park E; Cheon CH
[Ad] Endereço:Department of Chemistry, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, Republic of Korea. cheon@korea.ac.kr.
[Ti] Título:A general strategy for the synthesis of indoloquinolizine alkaloids via a cyanide-catalyzed imino-Stetter reaction.
[So] Source:Org Biomol Chem;15(48):10265-10275, 2017 Dec 13.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new strategy applicable to the synthesis of indoloquinolizine natural products has been developed. A cyanide-catalyzed intramolecular imino-Stetter reaction of aldimines, derived from 2-aminocinnamic acid derivatives and 2-pyridinecarboxaldehydes, provided indole-3-acetic acid derivatives bearing a pyridyl ring at the 2-position. Reduction of the carboxylic acid moiety to an alcohol followed by activation of the resulting alcohol with Tf O or TsCl generated indoloquinolizinium salts, which were utilized as precursors for indoloquinolizine natural products. The advantage of this protocol was successfully demonstrated in the total syntheses of arborescidine A and nauclefidine.
[Mh] Termos MeSH primário: Alcaloides/síntese química
Cianetos/química
Iminas/química
Quinolizinas/síntese química
[Mh] Termos MeSH secundário: Alcaloides/química
Catálise
Estrutura Molecular
Quinolizinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Cyanides); 0 (Imines); 0 (Quinolizines)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171130
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob02691a


  2 / 4707 MEDLINE  
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[PMID]:29273526
[Au] Autor:Stueber T; Meyer S; Jangra A; Hage A; Eberhardt M; Leffler A
[Ad] Endereço:Department of Anaesthesiology and Intensive Care Medicine, Hannover Medical School, Hannover, Germany.
[Ti] Título:Activation of the capsaicin-receptor TRPV1 by the acetaminophen metabolite N-arachidonoylaminophenol results in cytotoxicity.
[So] Source:Life Sci;194:67-74, 2018 Feb 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: The anandamide reuptake inhibitor N-arachidonoylaminophenol (AM404) and the reactive substance N-acetyl-p-benzoquinone imine (NAPQI) are both metabolites of acetaminophen and may contribute to acetaminophen-induced analgesia by acting at TRPV1 expressed in the peripheral or central nervous system. While NAPQI slowly sensitizes and activates TRPV1 by interacting with distinct intracellular cysteine residues, detailed properties of AM404 as an agonist of TRPV1 have not yet been reported on. We explored the effects of AM404 on recombinant human TRPV1 and in rodent dorsal root ganglion (DRG) neurons. MATERIALS AND METHODS: HEK 293 cells expressing different isoforms of recombinant TRPV1 and rodent DRG neurons were employed for patch clamp and calcium imaging experiments. Cytotoxicity was assessed by propidium iodide and Annexin V staining on TRPV1-HEK 293 cells and with trypan blue staining on DRG neurons. KEY FINDINGS: AM404 activates hTRPV1 at concentrations >1µM and in a concentration-dependent manner. AM404 also potentiates TRPV1-mediated currents evoked by heat and anandamide. Moreover, AM404-evoked currents are potentiated by NAPQI. While the partly capsaicin-insensitive rabbit (o) TRPV1 fails to respond to AM404, AM404-sensitivity is restored by insertion of the capsaicin binding-domain of rat TRPV1 into oTRPV1. In DRG neurons, AM404-evoked calcium influx as well as cell death is mediated by TRPV1. SIGNIFICANCE: AM404 gates TRPV1 by interacting with the vanilloid-binding site, and TRPV1 is the main receptor for AM404 in DRG neurons. While direct activation of TRPV1 requires high concentrations of AM404, it is possible that synergistic effects of AM404 with further TRPV1-agonists may occur at clinically relevant concentrations.
[Mh] Termos MeSH primário: Acetaminofen/farmacologia
Analgésicos não Entorpecentes/farmacologia
Ácidos Araquidônicos/farmacologia
Gânglios Espinais/efeitos dos fármacos
Canais de Cátion TRPV/metabolismo
[Mh] Termos MeSH secundário: Acetaminofen/metabolismo
Analgesia
Analgésicos não Entorpecentes/metabolismo
Animais
Ácidos Araquidônicos/metabolismo
Benzoquinonas/metabolismo
Capsaicina/farmacologia
Gânglios Espinais/citologia
Células HEK293
Seres Humanos
Iminas/metabolismo
Camundongos Endogâmicos C57BL
Neurônios/efeitos dos fármacos
Neurônios/metabolismo
Coelhos
Ratos Sprague-Dawley
Fármacos do Sistema Sensorial/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Arachidonic Acids); 0 (Benzoquinones); 0 (Imines); 0 (Sensory System Agents); 0 (TRPV Cation Channels); 0 (TRPV1 protein, human); 362O9ITL9D (Acetaminophen); G6S9BN13TI (N-acetyl-4-benzoquinoneimine); S07O44R1ZM (Capsaicin); XVJ94H0U21 (N-(4-hydroxyphenyl)arachidonylamide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171224
[St] Status:MEDLINE


  3 / 4707 MEDLINE  
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[PMID]:29179179
[Au] Autor:Shi R; Xiao ZT; Zheng YJ; Zhang YL; Xu JW; Huang JH; Zhou WL; Li PB; Su WW
[Ad] Endereço:Guangdong Engineering & Technology Research Center for Quality and Efficacy Re-evaluation of Post-market Traditional Chinese Medicine, School of Life Sciences, Sun Yat-sen University, Guangzhou, China.
[Ti] Título:Naringenin Regulates CFTR Activation and Expression in Airway Epithelial Cells.
[So] Source:Cell Physiol Biochem;44(3):1146-1160, 2017.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: Sputum symptoms are commonly seen in the elderly. This study aimed to identify an efficacious expectorant treatment stratagem through evaluating the secretion-promoting activation and cystic fibrosis transmembrane conductance regulator (CFTR) expression of the bioactive herbal monomer naringenin. METHODS: Vectorial Cl- transport was determined by measuring short-circuit current (ISC) in rat airway epithelium. cAMP content was measured by ELISA in primary cultured epithelial cells and Calu-3 cells. CFTR expression in Calu-3 cells was determined by qPCR. RESULTS: Addition of naringenin to the basolateral side of the rat airway led to a concentration-dependent sustained increase in ISC. The current was suppressed when exposed to Cl--free solution or by bumetanide, BaCl2, and DPC but not by DIDS and IBMX. Forskolin-induced ISC increase and CFTRinh-172/MDL-12330A-induced ISC inhibition were not altered by naringenin. Intracellular cAMP content was significantly increased by naringenin. With lipopolysaccharide stimulation, CFTR expression was significantly reduced, and naringenin dose-dependently enhanced CFTR mRNA expression. CONCLUSION: These results demonstrate that naringenin has the ability to stimulate Cl- secretion, which is mediated by CFTR through a signaling pathway by increasing cAMP content. Moreover, naringenin can increase CFTR expression when organism CFTR expression is seriously hampered. Our data suggest a potentially effective treatment strategy for sputum.
[Mh] Termos MeSH primário: Regulador de Condutância Transmembrana em Fibrose Cística/metabolismo
Células Epiteliais/efeitos dos fármacos
Flavanonas/farmacologia
[Mh] Termos MeSH secundário: Animais
Compostos de Bário/farmacologia
Benzoatos/farmacologia
Células Cultivadas
Canais de Cloreto/antagonistas & inibidores
Canais de Cloreto/metabolismo
Cloretos/farmacologia
Colforsina/farmacologia
AMP Cíclico/análise
Regulador de Condutância Transmembrana em Fibrose Cística/antagonistas & inibidores
Regulador de Condutância Transmembrana em Fibrose Cística/genética
Células Epiteliais/citologia
Células Epiteliais/metabolismo
Feminino
Seres Humanos
Iminas/farmacologia
Transporte de Íons/efeitos dos fármacos
Masculino
Microscopia de Fluorescência
Ratos
Ratos Sprague-Dawley
Reação em Cadeia da Polimerase em Tempo Real
Tiazolidinas/farmacologia
Traqueia/citologia
ortoaminobenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone); 0 (Barium Compounds); 0 (Benzoates); 0 (Chloride Channels); 0 (Chlorides); 0 (Flavanones); 0 (Imines); 0 (Thiazolidines); 0 (ortho-Aminobenzoates); 0VK51DA1T2 (barium chloride); 126880-72-6 (Cystic Fibrosis Transmembrane Conductance Regulator); 1F7A44V6OU (Colforsin); 82985-31-7 (RMI 12330A); 952VN06WBB (fenamic acid); E0399OZS9N (Cyclic AMP); HN5425SBF2 (naringenin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180118
[Lr] Data última revisão:
180118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1159/000485419


  4 / 4707 MEDLINE  
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[PMID]:28833946
[Au] Autor:Matzel P; Krautschick L; Höhne M
[Ad] Endereço:Protein Biochemistry, Institute of Biochemistry, University of Greifswald, Felix-Hausdorff-Strasse 4, 17487, Greifswald, Germany.
[Ti] Título:Photometric Characterization of the Reductive Amination Scope of the Imine Reductases from Streptomyces tsukubaensis and Streptomyces ipomoeae.
[So] Source:Chembiochem;18(20):2022-2027, 2017 Oct 18.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Imine reductases (IREDs) have emerged as promising enzymes for the asymmetric synthesis of secondary and tertiary amines starting from carbonyl substrates. Screening the substrate specificity of the reductive amination reaction is usually performed by time-consuming GC analytics. We found two highly active IREDs in our enzyme collection, IR-20 from Streptomyces tsukubaensis and IR-Sip from Streptomyces ipomoeae, that allowed a comprehensive substrate screening with a photometric NADPH assay. We screened 39 carbonyl substrates combined with 17 amines as nucleophiles. Activity data from 663 combinations provided a clear picture about substrate specificity and capabilities in the reductive amination of these enzymes. Besides aliphatic aldehydes, the IREDs accepted various cyclic (C -C ) and acyclic ketones, preferentially with methylamine. IR-Sip also accepted a range of primary and secondary amines as nucleophiles. In biocatalytic reactions, IR-Sip converted (R)-3-methylcyclohexanone with dimethylamine or pyrrolidine with high diastereoselectivity (>94-96 % de). The nucleophile acceptor spectrum depended on the carbonyl substrate employed. The conversion of well-accepted substrates could also be detected if crude lysates were employed as the enzyme source.
[Mh] Termos MeSH primário: Ensaios Enzimáticos
Iminas/metabolismo
Oxirredutases/metabolismo
Streptomyces/enzimologia
[Mh] Termos MeSH secundário: Aminação
NADP/metabolismo
Fotometria
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imines); 53-59-8 (NADP); EC 1.- (Oxidoreductases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170824
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700257


  5 / 4707 MEDLINE  
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[PMID]:28799763
[Au] Autor:Barresi E; Nesi G; Citi V; Piragine E; Piano I; Taliani S; Da Settimo F; Rapposelli S; Testai L; Breschi MC; Gargini C; Calderone V; Martelli A
[Ad] Endereço:Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6, 56126 Pisa, Italy.
[Ti] Título:Iminothioethers as Hydrogen Sulfide Donors: From the Gasotransmitter Release to the Vascular Effects.
[So] Source:J Med Chem;60(17):7512-7523, 2017 Sep 14.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The gasotransmitter hydrogen sulfide (H S) is an important tuner of the cardiovascular homeostasis, and its deficiency is etiologically associated with a number of cardiovascular diseases. Therefore, the research of original moieties able to release H S represents a timely issue for drug discovery. In this work, we developed a collection of iminothioethers (ITEs), exhibiting H S-releasing properties and producing vasorelaxing effects on rat aortic rings. Derivatives 4 and 11, selected as representative of slow and fast rate H S donors, respectively, produced a complete recovery of the basal coronary flow, reverting the AngII-induced effects in isolated rat hearts. In addition, studies on human aortic smooth muscle cells (HASMCs) demonstrated membrane hyperpolarizing effects, well related to the intracellular generation of H S. Taken together, the results obtained support ITEs 4 and 11 as new pharmacological tools, as well as effective and innovative H S donors for cardiovascular drug discovery.
[Mh] Termos MeSH primário: Gasotransmissores/farmacologia
Sulfeto de Hidrogênio/farmacologia
Sulfetos/farmacologia
Vasodilatadores/farmacologia
[Mh] Termos MeSH secundário: Animais
Aorta/efeitos dos fármacos
Aorta/fisiologia
Pressão Sanguínea/efeitos dos fármacos
Linhagem Celular
Descoberta de Drogas
Gasotransmissores/química
Seres Humanos
Sulfeto de Hidrogênio/química
Iminas/química
Iminas/farmacologia
Masculino
Miócitos de Músculo Liso/efeitos dos fármacos
Miócitos de Músculo Liso/metabolismo
Ratos
Ratos Wistar
Sulfetos/química
Vasodilatadores/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Gasotransmitters); 0 (Imines); 0 (Sulfides); 0 (Vasodilator Agents); YY9FVM7NSN (Hydrogen Sulfide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00888


  6 / 4707 MEDLINE  
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[PMID]:28757136
[Au] Autor:Divakar S; Saravanan K; Karthikeyan P; Elancheran R; Kabilan S; Balasubramanian KK; Devi R; Kotoky J; Ramanathan M
[Ad] Endereço:Department of Pharmacology, PSG College of Pharmacy, Coimbatore, Tamil Nadu, India.
[Ti] Título:Iminoenamine based novel androgen receptor antagonist exhibited anti-prostate cancer activity in androgen independent prostate cancer cells through inhibition of AKT pathway.
[So] Source:Chem Biol Interact;275:22-34, 2017 Sep 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Treatment by androgen receptor (AR) antagonists is one of the regimens for prostate cancer. The prolonged treatment with AR antagonist leads to the expression of point mutation in the ligand binding domain of the AR. This point mutation causes resistance to AR antagonist by converting them into an agonist. The T887A mutated AR was frequently expressed in androgen independent prostate cancer (AIPC) patients. Through literature survey and molecular modelling, we have identified a novel AR antagonist having a bulky ß-iminoenamine BF2 complex scaffold. The tested and standard ligands were screened in AR positive (LNCaP, MCF-7 and MDA-MB-453), AR negative (PC3), and non-cancerous (3T3) cell lines through anti-proliferation assay. The ligand, ARA3 was the most potent molecule among all the tested ligands and was 7.6 folds selective for AR positive cell lines. The mechanism of anti-prostate cancer activity of ARA3 was confirmed by western blot, qPCR, and apoptotic assays in LNCaP (T887A positive AR) cells. Structural activity relationship was derived by correlating the in-vitro and in-silico data. Consequently, we have identified the essential functional groups that could prevent the resistance concerning mutant AR. The ARA3 induces the apoptosis in AIPC cells by preventing the AR mediated activation of AKT pathway. The bicalutamide did not induce the apoptosis because it failed to prevent the AR mediated activation of AKT.
[Mh] Termos MeSH primário: Aminas/química
Aminas/farmacologia
Antagonistas de Receptores de Andrógenos/química
Neoplasias da Próstata/fisiopatologia
Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores
Receptores Androgênicos/metabolismo
[Mh] Termos MeSH secundário: Aminas/metabolismo
Antagonistas de Receptores de Andrógenos/metabolismo
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Sítios de Ligação
Caspase 3/metabolismo
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Seres Humanos
Iminas/química
Masculino
Microscopia de Fluorescência
Simulação de Acoplamento Molecular
Mutação
Neoplasias da Próstata/enzimologia
Proteínas Proto-Oncogênicas c-akt/genética
Proteínas Proto-Oncogênicas c-akt/metabolismo
Proteínas Proto-Oncogênicas c-bcl-2/metabolismo
Receptores Androgênicos/genética
Proteína X Associada a bcl-2/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (AR protein, human); 0 (Amines); 0 (Androgen Receptor Antagonists); 0 (Antineoplastic Agents); 0 (Imines); 0 (Proto-Oncogene Proteins c-bcl-2); 0 (Receptors, Androgen); 0 (bcl-2-Associated X Protein); EC 2.7.11.1 (AKT1 protein, human); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EC 3.4.22.- (Caspase 3)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170801
[St] Status:MEDLINE


  7 / 4707 MEDLINE  
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[PMID]:28722796
[Au] Autor:Roth S; Präg A; Wechsler C; Marolt M; Ferlaino S; Lüdeke S; Sandon N; Wetzl D; Iding H; Wirz B; Müller M
[Ad] Endereço:Institut für Pharmazeutische Wissenschaften, Albert-Ludwigs-Universität Freiburg, Albertstrasse 25, 79104, Freiburg, Germany.
[Ti] Título:Extended Catalytic Scope of a Well-Known Enzyme: Asymmetric Reduction of Iminium Substrates by Glucose Dehydrogenase.
[So] Source:Chembiochem;18(17):1703-1706, 2017 Sep 05.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:NADP(H)-dependent imine reductases (IREDs) are of interest in biocatalytic research due to their ability to generate chiral amines from imine/iminium substrates. In reaction protocols involving IREDs, glucose dehydrogenase (GDH) is generally used to regenerate the expensive cofactor NADPH by oxidation of d-glucose to gluconolactone. We have characterized different IREDs with regard to reduction of a set of bicyclic iminium compounds and have utilized H NMR and GC analyses to determine degree of substrate conversion and product enantiomeric excess (ee). All IREDs reduced the tested iminium compounds to the corresponding chiral amines. Blank experiments without IREDs also showed substrate conversion, however, thus suggesting an iminium reductase activity of GDH. This unexpected observation was confirmed by additional experiments with GDHs of different origin. The reduction of C=N bonds with good levels of conversion (>50 %) and excellent enantioselectivity (up to >99 % ee) by GDH represents a promiscuous catalytic activity of this enzyme.
[Mh] Termos MeSH primário: Glucose 1-Desidrogenase/metabolismo
Iminas/metabolismo
[Mh] Termos MeSH secundário: Bacillus subtilis/enzimologia
Biocatálise
Cromatografia Gasosa
Glucose/metabolismo
Iminas/química
Espectroscopia de Ressonância Magnética
NADP/metabolismo
Oxirredução
Estereoisomerismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imines); 53-59-8 (NADP); EC 1.1.1.47 (Glucose 1-Dehydrogenase); IY9XDZ35W2 (Glucose)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170720
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700261


  8 / 4707 MEDLINE  
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[PMID]:28640998
[Au] Autor:Kölmel DK; Kool ET
[Ad] Endereço:Department of Chemistry, Stanford University , Stanford, California 94305, United States.
[Ti] Título:Oximes and Hydrazones in Bioconjugation: Mechanism and Catalysis.
[So] Source:Chem Rev;117(15):10358-10376, 2017 Aug 09.
[Is] ISSN:1520-6890
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The formation of oximes and hydrazones is employed in numerous scientific fields as a simple and versatile conjugation strategy. This imine-forming reaction is applied in fields as diverse as polymer chemistry, biomaterials and hydrogels, dynamic combinatorial chemistry, organic synthesis, and chemical biology. Here we outline chemical developments in this field, with special focus on the past ∼10 years of developments. Recent strategies for installing reactive carbonyl groups and α-nucleophiles into biomolecules are described. The basic chemical properties of reactants and products in this reaction are then reviewed, with an eye to understanding the reaction's mechanism and how reactant structure controls rates and equilibria in the process. Recent work that has uncovered structural features and new mechanisms for speeding the reaction, sometimes by orders of magnitude, is discussed. We describe recent studies that have identified especially fast reacting aldehyde/ketone substrates and structural effects that lead to rapid-reacting α-nucleophiles as well. Among the most effective new strategies has been the development of substituents near the reactive aldehyde group that either transfer protons at the transition state or trap the initially formed tetrahedral intermediates. In addition, the recent development of efficient nucleophilic catalysts for the reaction is outlined, improving greatly upon aniline, the classical catalyst for imine formation. A number of uses of such second- and third-generation catalysts in bioconjugation and in cellular applications are highlighted. While formation of hydrazone and oxime has been traditionally regarded as being limited by slow rates, developments in the past 5 years have resulted in completely overturning this limitation; indeed, the reaction is now one of the fastest and most versatile reactions available for conjugations of biomolecules and biomaterials.
[Mh] Termos MeSH primário: Materiais Biocompatíveis/química
Materiais Biocompatíveis/síntese química
Hidrazonas/química
Oximas/química
[Mh] Termos MeSH secundário: Catálise
Iminas/síntese química
Iminas/química
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Biocompatible Materials); 0 (Hydrazones); 0 (Imines); 0 (Oximes)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171028
[Lr] Data última revisão:
171028
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170623
[St] Status:MEDLINE
[do] DOI:10.1021/acs.chemrev.7b00090


  9 / 4707 MEDLINE  
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[PMID]:28603976
[Au] Autor:Eftekhari-Sis B; Zirak M
[Ad] Endereço:Department of Chemistry, University of Maragheh , Maragheh 55181-83111, Iran.
[Ti] Título:α-Imino Esters in Organic Synthesis: Recent Advances.
[So] Source:Chem Rev;117(12):8326-8419, 2017 Jun 28.
[Is] ISSN:1520-6890
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:α-Imino esters are useful precursors for the synthesis of a variety of types of natural and unnatural α-amino acid derivatives, with a wide range of biological activities. Due to the adjacent ester group, α-imino esters are more reactive relative to other types of imines and undergo different kinds of reactions, including organometallics addition, metal catalyzed vinylation and alkynylation, aza-Henry, aza-Morita-Baylis-Hillman, imino-ene, Mannich-type, and cycloaddition reactions, as well as hydrogenation and reduction. This review discusses the mechanism, scope, and applications of the reactions of α-imino esters and related compounds in organic synthesis, covering the literature from the last 12 years.
[Mh] Termos MeSH primário: Técnicas de Química Sintética/métodos
Ésteres/química
Iminas/química
[Mh] Termos MeSH secundário: Catálise
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Esters); 0 (Imines)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170731
[Lr] Data última revisão:
170731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170613
[St] Status:MEDLINE
[do] DOI:10.1021/acs.chemrev.7b00064


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[PMID]:28581826
[Au] Autor:Safwat MA; Soliman GM; Sayed D; Attia MA
[Ad] Endereço:a Department of Pharmaceutics, Faculty of Pharmacy , Assiut University , Assiut , Egypt.
[Ti] Título:Gold nanoparticles capped with benzalkonium chloride and poly (ethylene imine) for enhanced loading and skin permeability of 5-fluorouracil.
[So] Source:Drug Dev Ind Pharm;43(11):1780-1791, 2017 Nov.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To enhance 5-fluorouracil (5-FU) permeability through the skin by loading onto gold nanoparticles (GNPs) capped with two cationic ligands, benzalkonium chloride (BC) or poly (ethylene imine) (PEI). Whereas 5-FU has excellent efficacy against many cancers, its poor permeability through biological membranes and several adverse effects limit its clinical benefits. BC and PEI were selected to stabilize GNPs and to load 5-FU through ionic interactions. METHODS: 5-FU/BC-GNPs and 5-FU/PEI-GNPs were prepared at different 5-FU/ligand molar ratios and different pH values and were evaluated using different techniques. GNPs stability was tested as a function of salt concentration and storage time. 5-FU release from BC- and PEI-GNPs was evaluated as a function of solution pH. Ex vivo permeability studies of different 5-FU preparations were carried out using mice skin. RESULTS: 5-FU-loaded GNPs size and surface charge were dependent on the 5-FU/ligand molar ratios. 5-FU entrapment efficiency and loading capacity were dependent on the used ligand, 5-FU/ligand molar ratio and solution pH. Maximum drug entrapment efficiency of 59.0 ± 1.7% and 46.0 ± 1.1% were obtained for 5-FU/BC-GNPs and 5-FU/PEI-GNPs, respectively. 5-FU-loaded GNPs had good stability against salinity and after storage for 4 months at room temperature and at 4 °C. In vitro 5-FU release was pH- and ligand-dependent where slower release was observed at higher pH and for 5-FU/BC-GNPs. 5-FU permeability through mice skin was significantly higher for drug-loaded GNPs compared with drug-ligand complex or drug aqueous solution. CONCLUSION: Based on these results, BC- and PEI-GNPs might find applications as effective topical delivery systems of 5-FU.
[Mh] Termos MeSH primário: Compostos de Benzalcônio/química
Compostos de Benzalcônio/metabolismo
Fluoruracila/administração & dosagem
Ouro/administração & dosagem
Ouro/química
Iminas/química
Nanopartículas/química
Polietilenos/química
[Mh] Termos MeSH secundário: Animais
Portadores de Fármacos
Fluoruracila/química
Seres Humanos
Camundongos
Nanopartículas/administração & dosagem
Permeabilidade
Pele
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzalkonium Compounds); 0 (Drug Carriers); 0 (Imines); 0 (Polyethylenes); 0 (poly(ethylene imine)); 7440-57-5 (Gold); U3P01618RT (Fluorouracil)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170606
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1339082



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