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[PMID]: 28461657 [Au] Autor: Green MR; Sambrook J [Ti] Título: Estimating the Concentration of DNA by Fluorometry Using Hoechst 33258. [So] Source: Cold Spring Harb Protoc;2017(5):pdb.prot093567, 2017 May 01. [Is] ISSN: 1559-6095 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Measuring the concentration of DNA using fluorometry is more sensitive than spectrophotometry, allowing the detection of nanogram quantities of DNA. In this assay, DNA preparations of known and unknown concentrations are incubated with the fluorochrome Hoechst 33258. Absorption values for the unknown sample are compared with those observed for a known dilution series, and the concentration of the unknown sample is estimated by interpolation. The assay can only be used to measure the concentration of DNAs whose sizes exceed ∼1 kb, as Hoechst 33258 binds poorly to smaller DNAs. [Mh] Termos MeSH primário: Bisbenzimidazol DNA/análise Corantes Fluorescentes Fluorometria/métodos [Mh] Termos MeSH secundário: Bisbenzimidazol/metabolismo DNA/metabolismo Indicadores e Reagentes Soluções [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Fluorescent Dyes); 0 (Indicators and Reagents); 0 (Solutions); 9007-49-2 (DNA); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180129 [Lr] Data última revisão: 180129 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170503 [St] Status: MEDLINE [do] DOI: 10.1101/pdb.prot093567

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[PMID]: 28659488 [Au] Autor: Yakimovich A; Huttunen M; Zehnder B; Coulter LJ; Gould V; Schneider C; Kopf M; McInnes CJ; Greber UF; Mercer J [Ad] Endereço: Institute of Molecular Life Sciences, University of Zurich, Zurich, Switzerland. [Ti] Título: Inhibition of Poxvirus Gene Expression and Genome Replication by Bisbenzimide Derivatives. [So] Source: J Virol;91(18), 2017 Sep 15. [Is] ISSN: 1098-5514 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Virus infection of humans and livestock can be devastating for individuals and populations, sometimes resulting in large economic and societal impact. Prevention of virus disease by vaccination or antiviral agents is difficult to achieve. A notable exception was the eradication of human smallpox by vaccination over 30 years ago. Today, humans and animals remain susceptible to poxvirus infections, including zoonotic poxvirus transmission. Here we identified a small molecule, bisbenzimide (bisbenzimidazole), and its derivatives as potent agents against prototypic poxvirus infection in cell culture. We show that bisbenzimide derivatives, which preferentially bind the minor groove of double-stranded DNA, inhibit vaccinia virus infection by blocking viral DNA replication and abrogating postreplicative intermediate and late gene transcription. The bisbenzimide derivatives are potent against vaccinia virus and other poxviruses but ineffective against a range of other DNA and RNA viruses. The bisbenzimide derivatives are the first inhibitors of their class, which appear to directly target the viral genome without affecting cell viability. Smallpox was one of the most devastating diseases in human history until it was eradicated by a worldwide vaccination campaign. Due to discontinuation of routine vaccination more than 30 years ago, the majority of today's human population remains susceptible to infection with poxviruses. Here we present a family of bisbenzimide (bisbenzimidazole) derivatives, known as Hoechst nuclear stains, with high potency against poxvirus infection. Results from a variety of assays used to dissect the poxvirus life cycle demonstrate that bisbenzimides inhibit viral gene expression and genome replication. These findings can lead to the development of novel antiviral drugs that target viral genomes and block viral replication. [Mh] Termos MeSH primário: Antivirais/farmacologia Bisbenzimidazol/farmacologia Replicação do DNA/efeitos dos fármacos Transcrição Genética/efeitos dos fármacos Vírus Vaccinia/efeitos dos fármacos Vírus Vaccinia/fisiologia Replicação Viral/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Linhagem Celular Corantes Fluorescentes Seres Humanos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antiviral Agents); 0 (Fluorescent Dyes); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170906 [Lr] Data última revisão: 170906 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170630 [St] Status: MEDLINE

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[PMID]: 28525298 [Au] Autor: Gholivand MB; Peyman H; Gholivand K; Roshanfekr H; Taherpour AA; Yaghoubi R [Ad] Endereço: 1 Faculty of Chemistry, Sensor and Biosensor Research Center (SBRC) and Nanoscience and Nanotechnology Research Center (NNRC), Razi University , Kermanshah, Iran . [Ti] Título: Experimental and Computational Evidence on the Interaction of Cycloalkyl α-Aminobisphosphonates with Calf Thymus DNA. [So] Source: DNA Cell Biol;36(7):541-551, 2017 Jul. [Is] ISSN: 1557-7430 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Fluorescence spectroscopy, ultraviolet-visible absorption spectroscopy, circular dichroism spectroscopy, viscometry, cyclic voltammetry, and differential pulse voltammetry were applied to investigate the competitive interaction of DNA with the three new cycloalkyl α-aminobisphosphonates (D -D ) and spectroscopic probe, neutral red dye, and Hoechst (HO), in a Tris-hydrogen chloride buffer (pH 7.4). The spectroscopic and voltammetric studies showed that the groove binding mode of interaction is predominant in the solution containing DNA and α-aminobisphosphonates. Furthermore, the results indicated that α-aminobisphosphonate with the lengthy N alkyl chains and larger heterocyclic ring size had a stronger interaction. The principal component analysis and theoretical quantum mechanical and molecular mechanics (QM-DFT B3LYP/6-31+G* and MM-SYBYL) methods were also applied to determine the number of chemical components presented in complexation equilibrium and identify the structure complexes of DNA with the three new cycloalkyl α-aminobisphosphonates (D -D ), respectively. [Mh] Termos MeSH primário: DNA/química Difosfonatos/química [Mh] Termos MeSH secundário: Animais Sítios de Ligação Ligação Competitiva Bisbenzimidazol/química Tampões (Química) Bovinos Técnicas Eletroquímicas Corantes Fluorescentes/química Cinética Vermelho Neutro/química Análise de Componente Principal Teoria Quântica Soluções Espectrometria de Fluorescência Termodinâmica [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Buffers); 0 (Diphosphonates); 0 (Fluorescent Dyes); 0 (Solutions); 261QK3SSBH (Neutral Red); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170920 [Lr] Data última revisão: 170920 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170520 [St] Status: MEDLINE [do] DOI: 10.1089/dna.2016.3624

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[PMID]: 28513176 [Au] Autor: Ranjan N; Story S; Fulcrand G; Leng F; Ahmad M; King A; Sur S; Wang W; Tse-Dinh YC; Arya DP [Ad] Endereço: Laboratory of Medicinal Chemistry, Department of Chemistry, Clemson University , Clemson, South Carolina 29634, United States. [Ti] Título: Selective Inhibition of Escherichia coli RNA and DNA Topoisomerase I by Hoechst 33258 Derived Mono- and Bisbenzimidazoles. [So] Source: J Med Chem;60(12):4904-4922, 2017 Jun 22. [Is] ISSN: 1520-4804 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: A series of Hoechst 33258 based mono- and bisbenzimidazoles have been synthesized and their Escherichia coli DNA topoisomerase I inhibition, binding to B-DNA duplex, and antibacterial activity has been evaluated. Bisbenzimidazoles with alkynyl side chains display excellent E. coli DNA topoisomerase I inhibition properties with IC values <5.0 µM. Several bisbenzimidazoles (3, 6, 7, 8) also inhibit RNA topoisomerase activity of E. coli DNA topoisomerase I. Bisbenzimidazoles inhibit bacterial growth much better than monobenzimidazoles for Gram-positive strains. The minimum inhibitory concentration (MIC) was much lower for Gram positive bacteria (Enterococcus spp. and Staphylococcus spp., including two MRSA strains 0.3-8 µg/mL) than for the majority of Gram negative bacteria (Pseudomonas aeruginosa, 16-32 µg/mL, Klebsiella pneumoniae > 32 µg/mL). Bisbenzimidazoles showed varied stabilization of B-DNA duplex (1.2-23.4 °C), and cytotoxicity studies show similar variation dependent upon the side chain length. Modeling studies suggest critical interactions between the inhibitor side chain and amino acids of the active site of DNA topoisomerase I. [Mh] Termos MeSH primário: Antibacterianos/farmacologia Benzimidazóis/farmacologia Bisbenzimidazol/química Escherichia coli/efeitos dos fármacos Inibidores da Topoisomerase I/farmacologia [Mh] Termos MeSH secundário: Antibacterianos/química Benzimidazóis/química Linhagem Celular Tumoral Técnicas de Química Sintética DNA/metabolismo Avaliação Pré-Clínica de Medicamentos/métodos Ensaios de Seleção de Medicamentos Antitumorais/métodos Escherichia coli/genética Proteínas de Escherichia coli/antagonistas & inibidores Seres Humanos Concentração Inibidora 50 Isomerases/antagonistas & inibidores Masculino Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos Testes de Sensibilidade Microbiana Simulação de Acoplamento Molecular Inibidores da Topoisomerase I/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Benzimidazoles); 0 (Escherichia coli Proteins); 0 (Topoisomerase I Inhibitors); 9007-49-2 (DNA); EC 5.- (Isomerases); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170811 [Lr] Data última revisão: 170811 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170518 [St] Status: MEDLINE [do] DOI: 10.1021/acs.jmedchem.7b00191

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[PMID]: 28296056 [Au] Autor: Korosh T; Bujans E; Morada M; Karaalioglu C; Vanden Eynde JJ; Mayence A; Huang TL; Yarlett N [Ad] Endereço: Department of Chemistry and Physical Sciences, Pace University, New York, NY, USA. [Ti] Título: Potential of bisbenzimidazole-analogs toward metronidazole-resistant Trichomonas vaginalis isolates. [So] Source: Chem Biol Drug Des;90(4):489-495, 2017 Oct. [Is] ISSN: 1747-0285 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A bisoxyphenylene-bisbenzimidazole series with increasing aliphatic chain length (CH to C H ) containing a meta- (m) or para (p)-benzimidazole linkage to the phenylene ring was tested for ability to inhibit the growth of metronidazole-susceptible (C1) and metronidazole-refractory (085) Trichomonas vaginalis isolates under aerobic and anaerobic conditions. Compound 3m, 2,2'-[α,ω-propanediylbis(oxy-1,3-phenylene)]bis-1H-benzimidazole, displayed a 5.5-fold lower minimum inhibitory concentration (MIC) toward T. vaginalis isolate 085 than metronidazole under aerobic growth conditions, (26 µm compared to 145 µm). A dose of 25 mg/kg per day for four days of compound 3m cured a subcutaneous mouse model infection using T. vaginalis isolates 286 (metronidazole susceptible) and 085 (metronidazole refractory). Compound 3m was weakly reduced by pyruvate:ferredoxin oxidoreductase, but unlike metronidazole was not dependent upon added ferredoxin. It is concluded from structure-activity relationships that there was no obvious trend based on the length of the central aliphatic chain, or the steric position of the bisbenzimidazole enabling prediction of biological activity. The compounds generally fulfill Lipinski's rile of five, indicating their potential as drug leads. [Mh] Termos MeSH primário: Antiprotozoários/química Antiprotozoários/uso terapêutico Bisbenzimidazol/análogos & derivados Bisbenzimidazol/uso terapêutico Resistência a Medicamentos Vaginite por Trichomonas/tratamento farmacológico Trichomonas vaginalis/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Antiprotozoários/farmacologia Bisbenzimidazol/farmacologia Linhagem Celular Tumoral Feminino Seres Humanos Metronidazol/farmacologia Camundongos Testes de Sensibilidade Microbiana Trichomonas vaginalis/crescimento & desenvolvimento [Pt] Tipo de publicação: EDITORIAL [Nm] Nome de substância: 0 (Antiprotozoal Agents); 140QMO216E (Metronidazole); LHQ7J5KV9B (Bisbenzimidazole) [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: 170316 [St] Status: MEDLINE [do] DOI: 10.1111/cbdd.12972

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[PMID]: 27835056 [Au] Autor: Shahabadi N; Shiri F [Ad] Endereço: a Inorganic Chemistry Department , Faculty of Chemistry, Razi University , Kermanshah , Iran. [Ti] Título: Multispectroscopic studies on the interaction of a copper(ii) complex of ibuprofen drug with calf thymus DNA. [So] Source: Nucleosides Nucleotides Nucleic Acids;36(2):83-106, 2017 Feb. [Is] ISSN: 1532-2335 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: The interaction of copper(II)-ibuprofenato complex with calf thymus DNA (ct-DNA) has been explored following, UV-visible spectrophotometry, fluorescence measurement, dynamic viscosity measurements, and circular dichroism spectroscopy. In spectrophotometric studies of ct-DNA it was found that [Cu(ibp) ] can form a complex with double-helical DNA. The association constant of [Cu(ibp) ] with DNA from UV-Vis study was found to be 6.19 × 10 L mol . The values of K from fluorescence measurement clearly underscore the high affinity of [Cu(ibp) ] to DNA. The experimental results showed that the conformational changes in DNA helix induced by [Cu(ibp) ] are the reason for the fluorescence quenching of the DNA-Hoechst system. In addition, the fluorescence emission spectra of intercalated methylene blue (MB) with increasing concentrations of [Cu(ibp) ] represented a significant increase of MB intensity as to release MB from MB-DNA system. The results of circular dichroism (CD) suggested that copper(II)-ibuprofenato complex can change the conformation of DNA. In addition, the results of viscosity measurements suggest that copper(II)-ibuprofenato complex may bind with non-classical intercalative mode. From spectroscopic and hydrodynamic studies, it has been found that [Cu(ibp) ] interacts with DNA by partial intercalation mode which contains intercalation and groove properties. [Mh] Termos MeSH primário: DNA/metabolismo Compostos Organometálicos/química Compostos Organometálicos/metabolismo [Mh] Termos MeSH secundário: Sítios de Ligação Ligação Competitiva Bisbenzimidazol/química Bisbenzimidazol/metabolismo Dicroísmo Circular DNA/química Fluorescência Substâncias Intercalantes/química Azul de Metileno/química Azul de Metileno/metabolismo Simulação de Acoplamento Molecular Conformação de Ácido Nucleico Espectrofotometria Ultravioleta Espectroscopia de Infravermelho com Transformada de Fourier Termodinâmica Viscosidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Intercalating Agents); 0 (Organometallic Compounds); 0 (tetrakis(ibuprofenato)dicopper(II)); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); LHQ7J5KV9B (Bisbenzimidazole); T42P99266K (Methylene Blue) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170310 [Lr] Data última revisão: 170310 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161112 [St] Status: MEDLINE [do] DOI: 10.1080/15257770.2016.1223305

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[PMID]: 27759493 [Au] Autor: Shahabadi N; Pourfoulad M; Moghadam NH [Ad] Endereço: a Department of Chemistry , Faculty of Science, Razi University , Kermanshah , Iran. [Ti] Título: Experimental and computational studies on the effects of valganciclovir as an antiviral drug on calf thymus DNA. [So] Source: Nucleosides Nucleotides Nucleic Acids;36(1):31-48, 2017 Jan 02. [Is] ISSN: 1532-2335 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: DNA-binding properties of an antiviral drug, valganciclovir (valcyte) was studied by using emission, absorption, circular dichroism, viscosity, differential pulse voltammetry, fluorescence techniques, and computational studies. The drug bound to calf thymus DNA (ct-DNA) in a groove-binding mode. The calculated binding constant of UV-vis, K , is comparable to groove-binding drugs. Competitive fluorimetric studies with Hoechst 33258 showed that valcyte could displace the DNA-bound Hoechst 33258. The drug could not displace intercalated methylene blue from DNA double helix. Furthermore, the induced detectable changes in the CD spectrum of ct-DNA as well as changes in its viscosity confirm the groove-binding mode. In addition, an integrated molecular docking was employed to further investigate the binding interactions between valcyte and calf thymus DNA. [Mh] Termos MeSH primário: DNA/química DNA/metabolismo Ganciclovir/análogos & derivados [Mh] Termos MeSH secundário: Antivirais/química Antivirais/metabolismo Sítios de Ligação Ligação Competitiva Bisbenzimidazol/química Dicroísmo Circular Eletroquímica/métodos Ganciclovir/química Ganciclovir/metabolismo Substâncias Intercalantes/química Azul de Metileno/química Azul de Metileno/metabolismo Simulação de Acoplamento Molecular Conformação de Ácido Nucleico Espectrometria de Fluorescência Termodinâmica Viscosidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antiviral Agents); 0 (Intercalating Agents); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); GCU97FKN3R (valganciclovir); LHQ7J5KV9B (Bisbenzimidazole); P9G3CKZ4P5 (Ganciclovir); T42P99266K (Methylene Blue) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170306 [Lr] Data última revisão: 170306 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161021 [St] Status: MEDLINE [do] DOI: 10.1080/15257770.2016.1218019

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[PMID]: 27891207 [Au] Autor: Su M; Yu T; Zhang H; Wu Y; Wang X; Li G [Ad] Endereço: Department of Pharmacology, Pharmacy School, Inner Mongolian Medical University, Jinshan Developing Zone, Hohhot, Inner Mongolia 010110, China. [Ti] Título: The Antiapoptosis Effect of Glycyrrhizate on HepG2 Cells Induced by Hydrogen Peroxide. [So] Source: Oxid Med Cell Longev;2016:6849758, 2016. [Is] ISSN: 1942-0994 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: This study demonstrated that glycyrrhizate (GAS) could protect HEPG2 cells against damage and apoptosis induced by H O (1600 M, 4 h). Cell viability assay revealed that GAS was noncytotoxity at concentration 125 g/mL, and GAS (5 g/mL, 25 g/mL, and 125 g/mL) protected HepG2 cells against H O -induced cytotoxicity. H O induced the HepG2 cells apoptosis, obvious morphologic changes were observed after Hochest 33258 staining, and more apoptotic cells were counted in flow cytometry assay compared to that of the natural group. Pretreatment GAS (5 g/mL, 25 g/mL, and 125 g/mL) prior to H O reverses the morphologic changes and reduced the apoptotic cells in HepG2 cells. GAS reduced the release of MDA, increased the activities of superoxide dismutase, and diminished the release of ALT and AST during oxidative stress in HepG2 cells. After Elisa kit detecting, GAS inhibited the caspase activity induced by H O , GAS decreased the level of caspase-3 and caspase-9 from mitochondria in dose-dependent manner. Western blot results showed that pretreatment GAS upregulated the expression of Bcl-2 and decreased the expression of Bax. These results reveal that GAS has the cytoprotection in HepG2 cells during ROS exposure by inhibiting the caspase activity in the mitochondria and influencing apoptogenic factors of the expression of Bax and Bcl-2. [Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos Ácido Glicirrízico/farmacologia Peróxido de Hidrogênio/toxicidade [Mh] Termos MeSH secundário: Alanina Transaminase/metabolismo Aspartato Aminotransferases/metabolismo Bisbenzimidazol/metabolismo Caspases/metabolismo Ativação Enzimática/efeitos dos fármacos Células Hep G2 Seres Humanos Peroxidação de Lipídeos/efeitos dos fármacos Malondialdeído/metabolismo Coloração e Rotulagem Superóxido Dismutase/metabolismo Proteína X Associada a bcl-2/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (bcl-2-Associated X Protein); 4Y8F71G49Q (Malondialdehyde); 6FO62043WK (Glycyrrhizic Acid); BBX060AN9V (Hydrogen Peroxide); EC 1.15.1.1 (Superoxide Dismutase); EC 2.6.1.1 (Aspartate Aminotransferases); EC 2.6.1.2 (Alanine Transaminase); EC 3.4.22.- (Caspases); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170313 [Lr] Data última revisão: 170313 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161129 [St] Status: MEDLINE

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[PMID]: 27884695 [Au] Autor: Ranjan N; Arya DP [Ad] Endereço: Laboratory of Bioorganic and Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, United States. [Ti] Título: Linker dependent intercalation of bisbenzimidazole-aminosugars in an RNA duplex; selectivity in RNA vs. DNA binding. [So] Source: Bioorg Med Chem Lett;26(24):5989-5994, 2016 12 15. [Is] ISSN: 1464-3405 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Neomycin and Hoechst 33258 are two well-known nucleic acid binders that interact with RNA and DNA duplexes with high affinities respectively. In this manuscript, we report that covalent attachment of bisbenzimidazole unit derived from Hoechst 33258 to neomycin leads to intercalative binding of the bisbenzimidazole unit (oriented at 64-74° with respected to the RNA helical axis) in a linker length dependent manner. The dual binding and intercalation of conjugates were supported by thermal denaturation, CD, LD and UV-Vis absorption experiments. These studies highlight the importance of linker length in dual recognition by conjugates, for effective RNA recognition, which can lead to novel ways of recognizing RNA structures. Additionally, the ligand library screens also identify DNA and RNA selective compounds, with compound 9, containing a long linker, showing a 20.3°C change in RNA duplex T with only a 13.0°C change in T for the corresponding DNA duplex. Significantly, the shorter linker in compound 3 shows almost the reverse trend, a 23.8°C change in DNA T , with only a 9.1°C change in T for the corresponding RNA duplex. [Mh] Termos MeSH primário: Amino Açúcares/farmacologia Bisbenzimidazol/farmacologia DNA/efeitos dos fármacos RNA/efeitos dos fármacos [Mh] Termos MeSH secundário: Amino Açúcares/química Sítios de Ligação/efeitos dos fármacos Bisbenzimidazol/química Relação Dose-Resposta a Droga Ligantes Estrutura Molecular Relação Estrutura-Atividade Temperatura Ambiente [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL [Nm] Nome de substância: 0 (Amino Sugars); 0 (Ligands); 63231-63-0 (RNA); 9007-49-2 (DNA); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 171124 [Lr] Data última revisão: 171124 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161126 [St] Status: MEDLINE

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[PMID]: 27576293 [Au] Autor: Özil M; Emirik M; Beldüz A; Ülker S [Ad] Endereço: Department of Chemistry, Recep Tayyip Erdogan University, 53100 Rize, Turkey. Electronic address: musa.ozil@erdogan.edu.tr. [Ti] Título: Molecular docking studies and synthesis of novel bisbenzimidazole derivatives as inhibitors of α-glucosidase. [So] Source: Bioorg Med Chem;24(21):5103-5114, 2016 Nov 01. [Is] ISSN: 1464-3391 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A series of bisbenzimidazole derivatives starting from o-phenylenediamine and 4-nitro-o-phenylenediamine were prepared with oxalic acid. Most of the reactions were conducted using both the microwave and conventional methods to compare yields and reaction times. The operational simplicity, environmental friendly conditions and high yield in a significantly short reaction time were the major benefits. All substances' inhibitory activities against α-glucosidase were evaluated. The results may suggest a significant role for the nature of bisbenzimidazole compounds in their inhibitory action against α-glucosidase. They showed different range of α-glucosidase inhibitory potential with IC value ranging between 0.44±0.04 and 6.69±0.01µM when compared to the standard acarbose (IC , 13.34±1.26µM). This has described a new class of α-glucosidase inhibitors. Molecular docking studies were done for all compounds to identify important binding modes responsible for inhibition activity of α-glucosidase. [Mh] Termos MeSH primário: Bisbenzimidazol/farmacologia Inibidores de Glicosídeo Hidrolases/farmacologia Simulação de Acoplamento Molecular alfa-Glucosidases/metabolismo [Mh] Termos MeSH secundário: Bisbenzimidazol/síntese química Bisbenzimidazol/química Relação Dose-Resposta a Droga Inibidores de Glicosídeo Hidrolases/síntese química Inibidores de Glicosídeo Hidrolases/química Seres Humanos Intestinos/enzimologia Estrutura Molecular Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Glycoside Hydrolase Inhibitors); EC 3.2.1.20 (alpha-Glucosidases); LHQ7J5KV9B (Bisbenzimidazole) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170919 [Lr] Data última revisão: 170919 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160901 [St] Status: MEDLINE

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2	and or and not		PalavrasDescritor de assuntoDescritor de assunto primárioLimitesAutorPalavras do títuloPalavras do resumoIdiomaPaís de publicaçãoNome de substânciaNome de pessoa como assuntoRevistaAssunto de RevistaISSNTipo de publicaçãoIdentificador únicoMês de entradaAno de publicaçãoTexto completoAtualização por classeCategoria DeCSCategoria DeCS explodidaCategoria CID-10SubSetsPais de AfiliaçãoAfiliaçãoAfiliação 2
3	and or and not		PalavrasDescritor de assuntoDescritor de assunto primárioLimitesAutorPalavras do títuloPalavras do resumoIdiomaPaís de publicaçãoNome de substânciaNome de pessoa como assuntoRevistaAssunto de RevistaISSNTipo de publicaçãoIdentificador únicoMês de entradaAno de publicaçãoTexto completoAtualização por classeCategoria DeCSCategoria DeCS explodidaCategoria CID-10SubSetsPais de AfiliaçãoAfiliaçãoAfiliação 2

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