Base de dados : MEDLINE
Pesquisa : D08.811.520.241.300.150 [Categoria DeCS]
Referências encontradas : 7202 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 721 ir para página                         

  1 / 7202 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29311545
[Au] Autor:Chrachri A; Hopkinson BM; Flynn K; Brownlee C; Wheeler GL
[Ad] Endereço:Marine Biological Association, Plymouth, PL1 2PB, UK.
[Ti] Título:Dynamic changes in carbonate chemistry in the microenvironment around single marine phytoplankton cells.
[So] Source:Nat Commun;9(1):74, 2018 01 08.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Photosynthesis by marine diatoms plays a major role in the global carbon cycle, although the precise mechanisms of dissolved inorganic carbon (DIC) uptake remain unclear. A lack of direct measurements of carbonate chemistry at the cell surface has led to uncertainty over the underlying membrane transport processes and the role of external carbonic anhydrase (eCA). Here we identify rapid and substantial photosynthesis-driven increases in pH and [CO ] primarily due to the activity of eCA at the cell surface of the large diatom Odontella sinensis using direct simultaneous microelectrode measurements of pH and CO along with modelling of cell surface inorganic carbonate chemistry. Our results show that eCA acts to maintain cell surface CO concentrations, making a major contribution to DIC supply in O. sinensis. Carbonate chemistry at the cell surface is therefore highly dynamic and strongly dependent on cell size, morphology and the carbonate chemistry of the bulk seawater.
[Mh] Termos MeSH primário: Carbonatos/metabolismo
Microambiente Celular
Diatomáceas/metabolismo
Fitoplâncton/metabolismo
[Mh] Termos MeSH secundário: Transporte Biológico
Carbono/química
Carbono/metabolismo
Dióxido de Carbono/química
Dióxido de Carbono/metabolismo
Carbonatos/química
Anidrases Carbônicas/metabolismo
Diatomáceas/citologia
Concentração de Íons de Hidrogênio
Modelos Biológicos
Fotossíntese
Fitoplâncton/citologia
Água do Mar/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Carbonates); 142M471B3J (Carbon Dioxide); 7440-44-0 (Carbon); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180110
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02426-y


  2 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28455260
[Au] Autor:Mikolajczyk-Stecyna J; Malinowska AM; Chmurzynska A
[Ad] Endereço:Molecular Metabolism Laboratory, Department of Human Nutrition and Hygiene, Faculty of Food Sciences, Poznan University of Life Sciences, Wojska Polskiego 31, 60-624 Poznan, Poland. Electronic address: joanstec@up.poznan.pl.
[Ti] Título:TAS2R38 and CA6 genetic polymorphisms, frequency of bitter food intake, and blood biomarkers among elderly woman.
[So] Source:Appetite;116:57-64, 2017 09 01.
[Is] ISSN:1095-8304
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Taste sensitivity is one of the most important biological determinants of food choice. Three SNPs of the TAS2R38 gene (rs713598, rs1726866, and rs10246939) give rise to two common haplotypes: PAV and AVI. These haplotypes, as well as an SNP within the CA6 gene (rs2274333) that encodes carbonic anhydrase VI (CA6), correlate with bitterness perception. The extent of consumption of bitter food may influence some health outcomes. The aim of this study is thus to investigate the impact of the TAS2R38 and CA6 genetic polymorphisms on the choice of bitter food, BMI, blood lipoprotein, and glucose concentrations as well as systemic inflammation in elderly women. METHODS: The associations between the TAS2R38 diplotype, CA6 genotype, and the intake of bitter-tasting foods were studied in a group of 118 Polish women over 60 years of age. The intake of Brassica vegetables, grapefruit, and coffee was assessed using a food frequency questionnaire. Biochemical parameters were measured using the spectrophotometric method. Genotyping was performed using the high resolution melting method. RESULTS: We found a correlation between lipid profile, glucose and CRP levels, and frequency of bitter food intake. The AVI/AVI subjects drank coffee more frequently than did the PAV/PAV homozygotes, as did the A carriers of CA6 in comparison with the GG homozygotes. We also observed that simultaneous carriers of the PAV haplotype and A allele of TAS2R38 and CA6, respectively, choose white cabbage more frequent and had lower plasma levels of CRP and glucose than did AVI/AVI and GG homozygotes. CONCLUSIONS: In elderly women, the TAS2R38 and CA6 polymorphisms may affect the frequency of consumption of coffee and white cabbage, but not of other bitter-tasting foods.
[Mh] Termos MeSH primário: Anidrases Carbônicas/genética
Fenômenos Fisiológicos da Nutrição do Idoso
Preferências Alimentares
Polimorfismo de Nucleotídeo Único
Receptores Acoplados a Proteínas-G/genética
Percepção Gustatória/genética
[Mh] Termos MeSH secundário: Idoso
Alelos
Biomarcadores/sangue
Brassica
Anidrases Carbônicas/metabolismo
Citrus paradisi
Café
Feminino
Frutas
Frequência do Gene
Estudos de Associação Genética
Seres Humanos
Meia-Idade
Polônia
Receptores Acoplados a Proteínas-G/metabolismo
Autorrelato
Paladar
Verduras
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Coffee); 0 (Receptors, G-Protein-Coupled); 0 (taste receptors, type 2); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase VI)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170430
[St] Status:MEDLINE


  3 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29390912
[Au] Autor:Supuran CT
[Ad] Endereço:a Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Florence , Italy.
[Ti] Título:Carbon- versus sulphur-based zinc binding groups for carbonic anhydrase inhibitors?
[So] Source:J Enzyme Inhib Med Chem;33(1):485-495, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A set of compounds incorporating carbon-based zinc-binding groups (ZBGs), of the type PhX (X = COOH, CONH , CONHNH , CONHOH, CONHOMe), and the corresponding derivatives with sulphur(VI)-based ZBGs (X = SO H, SO NH , SO NHNH , SO NHOH, SO NHOMe) were tested as inhibitors of all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1), CA I-XV. Three factors connected with the ZBG influenced the efficacy as CA inhibitor (CAI) of the investigated compounds: (i) the pKa of the ZBG; (ii) its geometry (tetrahedral, i.e. sulphur-based, versus trigonal, i.e. carbon-based ZBGs), and (iii) orientation of the organic scaffold induced by the nature of the ZBG. Benzenesulphonamide was the best inhibitor of all isoforms, but other ZBGs led to interesting inhibition profiles, although with an efficacy generally reduced when compared to the sulphonamide. The nature of the ZBG also influenced the CA inhibition mechanism. Most of these derivatives were zinc binders, but some of them (sulfonates, carboxylates) may interact with the enzyme by anchoring to the zinc-coordinated water molecule or by other inhibition mechanisms (occlusion of the active site entrance, out of the active site binding, etc.). Exploring structurally diverse ZBGs may lead to interesting new developments in the field of CAIs.
[Mh] Termos MeSH primário: Carbono/farmacologia
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Compostos Organometálicos/farmacologia
Enxofre/farmacologia
Zinco/farmacologia
[Mh] Termos MeSH secundário: Carbono/química
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Estrutura Molecular
Compostos Organometálicos/síntese química
Compostos Organometálicos/química
Relação Estrutura-Atividade
Enxofre/química
Zinco/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Organometallic Compounds); 70FD1KFU70 (Sulfur); 7440-44-0 (Carbon); EC 4.2.1.1 (Carbonic Anhydrases); J41CSQ7QDS (Zinc)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180203
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1428572


  4 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29363370
[Au] Autor:Vullo D; Lehneck R; Pöggeler S; Supuran CT
[Ad] Endereço:a Polo Scientifico, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze , Sesto Fiorentino, Florence , Italy.
[Ti] Título:Sulfonamide inhibition studies of two ß-carbonic anhydrases from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2.
[So] Source:J Enzyme Inhib Med Chem;33(1):390-396, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The two ß-carbonic anhydrases (CAs, EC 4.2.1.1) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was efficiently inhibited by tosylamide, 3-fluorosulfanilamide, and 3-chlorosulfanilamide (K s in the range of 43.2-79.6 nM), whereas acetazolamide, methazolamide, topiramate, ethoxzolamide, dorzolamide, and brinzolamide were medium potency inhibitors (K s in the range of 360-445 nM). CAS2 was less sensitive to sulfonamide inhibitors. The best CAS2 inhibitors were 5-amino-1,3,4-thiadiazole-2-sulfonamide (the deacetylated acetazolamide precursor) and 4-hydroxymethyl-benzenesulfonamide, with K s in the range of 48.1-92.5 nM. Acetazolamide, dorzolamide, ethoxzolamide, topiramate, sulpiride, indisulam, celecoxib, and sulthiame were medium potency CAS2 inhibitors (K s of 143-857 nM). Many other sulfonamides showed affinities in the high micromolar range or were ineffective as CAS1/2 inhibitors. Small changes in the structure of the inhibitor led to important differences of the activity. As these enzymes may show applications for the removal of anthropically generated polluting gases, finding modulators of their activity may be crucial for designing environmental-friendly CO capture processes.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Hifas/enzimologia
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Estrutura Molecular
Relação Estrutura-Atividade
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Sulfonamides); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180125
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1425687


  5 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29322852
[Au] Autor:Vullo D; Syrjänen L; Kuuslahti M; Parkkila S; Supuran CT
[Ad] Endereço:a Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica , Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.
[Ti] Título:Anion inhibition studies of a beta carbonic anhydrase from the malaria mosquito Anopheles gambiae.
[So] Source:J Enzyme Inhib Med Chem;33(1):359-363, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:An anion inhibition study of the ß-class carbonic anhydrase, AgaCA, from the malaria mosquito Anopheles gambiae is reported. A series of simple as well as complex inorganic anions, and small molecules known to interact with CAs were included in the study. Bromide, iodide, bisulphite, perchlorate, perrhenate, perruthenate, and peroxydisulphate were ineffective AgaCA inhibitors, with K s > 200 mM. Fluoride, chloride, cyanate, thiocyanate, cyanide, bicarbonate, carbonate, nitrite, nitrate, sulphate, stannate, selenate, tellurate, diphosphate, divanadate, tetraborate, selenocyanide, and trithiocarbonate showed K s in the range of 1.80-9.46 mM, whereas N,N-diethyldithiocarbamate was a submillimolar AgaCA inhibitor (K of 0.65 mM). The most effective AgaCA inhibitors were sulphamide, sulphamic acid, phenylboronic acid and phenylarsonic acid, with inhibition constants in the range of 21-84 µM. The control of insect vectors responsible of the transmission of many protozoan diseases is rather difficult nowadays, and finding agents which can interfere with these processes, as the enzyme inhibitors investigated here, may arrest the spread of these diseases worldwide.
[Mh] Termos MeSH primário: Anopheles/enzimologia
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
[Mh] Termos MeSH secundário: Animais
Ânions/síntese química
Ânions/química
Ânions/farmacologia
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anions); 0 (Carbonic Anhydrase Inhibitors); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180115
[Lr] Data última revisão:
180115
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1421182


  6 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29322836
[Au] Autor:Angeli A; Del Prete S; Osman SM; Alasmary FAS; AlOthman Z; Donald WA; Capasso C; Supuran CT
[Ad] Endereço:a Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Florence , Italy.
[Ti] Título:Activation studies with amines and amino acids of the ß-carbonic anhydrase encoded by the Rv3273 gene from the pathogenic bacterium Mycobacterium tuberculosis.
[So] Source:J Enzyme Inhib Med Chem;33(1):364-369, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The activation of a ß-class carbonic anhydrase (CAs, EC 4.2.1.1) from Mycobacterium tuberculosis, encoded by the gene Rv3273 (mtCA 3), was investigated using a panel of natural and non-natural amino acids and amines. mtCA 3 was effectively activated by D-DOPA, L-Trp, dopamine and serotonin, with K s ranging between 8.98 and 12.1 µM. L-His and D-Tyr showed medium potency activating effects, with K s in the range of 17.6-18.2 µM, whereas other amines and amino acids were relatively ineffective activators, with K s in the range of 28.9-52.2 µM. As the physiological roles of the three mtCAs present in this pathogen are currently poorly understood and considering that inhibition of these enzymes has strong antibacterial effects, discovering molecules that modulate their enzymatic activity may lead to a better understanding of the factors related to the invasion and colonisation of the host during Mycobacterium tuberculosis infection.
[Mh] Termos MeSH primário: Aminas/metabolismo
Aminoácidos/química
Aminoácidos/metabolismo
Anidrases Carbônicas/genética
Anidrases Carbônicas/metabolismo
Mycobacterium tuberculosis/enzimologia
[Mh] Termos MeSH secundário: Aminas/química
Estrutura Molecular
Mycobacterium tuberculosis/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Amino Acids); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180115
[Lr] Data última revisão:
180115
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1422250


  7 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29216562
[Au] Autor:Mandalapu D; Kushwaha B; Gupta S; Krishna S; Srivastava N; Shukla M; Singh P; Chauhan BS; Goyani R; Maikhuri JP; Sashidhara KV; Kumar B; Tripathi R; Shukla PK; Siddiqi MI; Lal J; Gupta G; Sharma VL
[Ad] Endereço:Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Sitapur Road, Lucknow 226031, India.
[Ti] Título:Substituted carbamothioic amine-1-carbothioic thioanhydrides as novel trichomonicidal fungicides: Design, synthesis, and biology.
[So] Source:Eur J Med Chem;143:632-645, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Sexually transmitted diseases like trichomoniasis along with opportunistic fungal infections like candidiasis are major global health burden in female reproductive health. In this context a novel non-nitroimidazole class of substituted carbamothioic amine-1-carbothioic thioanhydride series was designed, synthesized, evaluated for trichomonacidal and fungicidal activities, and was found to be more active than the standard drug Metronidazole (MTZ). Compounds were trichomonicidal in the MIC ranges of 4.77-294.1 µM and 32.46-735.20 µM against MTZ-susceptible and -resistant strains, respectively. Further, compounds inhibited the growth of at least two out of ten fungal strains tested at MIC of 7.50-240.38 µM. The most active compound (20) of this series was 3.8 and 9.5 fold more active than the MTZ against the two Trichomonas strains tested. Compound 20 also significantly inhibited the sulfhydryl groups present over Trichomonas vaginalis and was found to be more active than the MTZ in vivo. Further, a docking analysis carried out with cysteine proteases supported their thiol inhibiting ability and preliminary pharmacokinetic study has shown good distribution and systemic clearance.
[Mh] Termos MeSH primário: Anidrases Carbônicas/farmacologia
Desenho de Drogas
Fungicidas Industriais/farmacologia
Compostos de Sulfidrila/farmacologia
Trichomonas/efeitos dos fármacos
[Mh] Termos MeSH secundário: Anidrases Carbônicas/síntese química
Anidrases Carbônicas/química
Relação Dose-Resposta a Droga
Fungicidas Industriais/síntese química
Fungicidas Industriais/química
Metronidazol/química
Metronidazol/farmacologia
Estrutura Molecular
Testes de Sensibilidade Parasitária
Relação Estrutura-Atividade
Compostos de Sulfidrila/síntese química
Compostos de Sulfidrila/química
Trichomonas/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fungicides, Industrial); 0 (Sulfhydryl Compounds); 140QMO216E (Metronidazole); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180110
[Lr] Data última revisão:
180110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE


  8 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29280407
[Au] Autor:Angeli A; Chiaramonte N; Manetti D; Romanelli MN; Supuran CT
[Ad] Endereço:a Dipartimento Neurofarba , Università degli Studi di Firenze, Sezione di Scienze Farmaceutiche e Nutraceutiche , Sesto Fiorentino (Florence) , Italy.
[Ti] Título:Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators.
[So] Source:J Enzyme Inhib Med Chem;33(1):303-308, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Four human (h) carbonic anhydrase isoforms (CA, EC 4.2.1.1), hCA I, II, IV, and VII, were investigated for their activation profile with piperazines belonging to various classes, such as N-aryl-, N-alkyl-, N-acyl-piperazines as well as 2,4-disubstituted derivatives. As the activation mechanism involves participation of the activator in the proton shuttling between the zinc-coordinated water molecule and the external milieu, these derivatives possessing diverse basicity and different scaffolds were appropriate for being investigated as CA activators (CAAs). Most of these derivatives showed CA activating properties against hCA I, II, and VII (cytosolic isoforms) but were devoid of activity against the membrane-associated hCA IV. For hCA I, the K s were in the range of 32.6-131 µM; for hCA II of 16.2-116 µM, and for hCA VII of 17.1-131 µM. The structure-activity relationship was intricate and not easy to rationalize, but the most effective activators were 1-(2-piperidinyl)-piperazine (K of 16.2 µM for hCA II), 2-benzyl-piperazine (K of 17.1 µM for hCA VII), and 1-(3-benzylpiperazin-1-yl)propan-1-one (K of 32.6 µM for hCA I). As CAAs may have interesting pharmacologic applications in cognition and for artificial tissue engineering, investigation of new classes of activators may be crucial for this relatively new research field.
[Mh] Termos MeSH primário: Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica IV/antagonistas & inibidores
Anidrase Carbônica I/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Piperazinas/farmacologia
[Mh] Termos MeSH secundário: Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Piperazinas/síntese química
Piperazinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Piperazines); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (CA4 protein, human); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase VI)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180105
[Lr] Data última revisão:
180105
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171228
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1417277


  9 / 7202 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29278948
[Au] Autor:Nocentini A; Cadoni R; Dumy P; Supuran CT; Winum JY
[Ad] Endereço:a Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier , Montpellier Cedex , France.
[Ti] Título:Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles.
[So] Source:J Enzyme Inhib Med Chem;33(1):286-289, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the ß-CA LdcCA versus the α-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen's carbonic anhydrases.
[Mh] Termos MeSH primário: Antiprotozoários/farmacologia
Compostos de Boro/farmacologia
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Compostos Heterocíclicos com 2 Anéis/farmacologia
Leishmania donovani/efeitos dos fármacos
Trypanosoma cruzi/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antiprotozoários/síntese química
Antiprotozoários/química
Compostos de Boro/síntese química
Compostos de Boro/química
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Compostos Heterocíclicos com 2 Anéis/síntese química
Compostos Heterocíclicos com 2 Anéis/química
Leishmania donovani/enzimologia
Testes de Sensibilidade Microbiana
Estrutura Molecular
Relação Estrutura-Atividade
Trypanosoma cruzi/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Boron Compounds); 0 (Carbonic Anhydrase Inhibitors); 0 (Heterocyclic Compounds, 2-Ring); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180105
[Lr] Data última revisão:
180105
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171228
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1414808


  10 / 7202 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29197732
[Au] Autor:De Luca L; Mancuso F; Ferro S; Buemi MR; Angeli A; Del Prete S; Capasso C; Supuran CT; Gitto R
[Ad] Endereço:Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali (CHIBIOFARAM), Università degli Studi di Messina, Viale Annunziata, I-98168 Messina, Italy. Electronic address: ldeluca@unime.it.
[Ti] Título:Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases.
[So] Source:Eur J Med Chem;143:276-282, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Coumarin derivatives are a peculiar class of inhibitors of the family of metalloenzymes carbonic anhydrases (CA, EC 4.2.1.1). Several coumarins display higher affinity and selectivity toward most relevant and druggable CA isoforms. By decorating the natural compound umbelliferone (1) we have identified a new series of coumarin-based compounds demonstrating high CA inhibitory effects with nanomolar affinity for hCA IX and hCA XII isoforms that were considered a target amenable to develop antitumor agents. The most active tested compounds proved to be potent inhibitors with K values equal to that of the well-known inhibitor acetazolamide (AAZ), that lacks selectivity over ubiquitous hCA I and hCA II. As suggested by docking studies the coumarins, that are lacking of the canonical metal binding groups, do not interact with Zinc ion within the catalytic site as found for classical sulfonamide type inhibitors of CAs. Thus, the studied inhibitors might possess a non-classical inhibitory mode of action preventing the carbon dioxide to entry into catalytic cavity and its conversion into bicarbonate ion. Specifically, the most active inhibitor of hCA XII compound 18i (K value of 5.5 nM) and its supposed hydrolytic products could establish a web of H-bond interactions within the enzymatic cavity.
[Mh] Termos MeSH primário: Anidrase Carbônica IX/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Cumarínicos/farmacologia
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/metabolismo
Anidrase Carbônica IX/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Cumarínicos/síntese química
Cumarínicos/química
Relação Dose-Resposta a Droga
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Carbonic Anhydrase Inhibitors); 0 (Coumarins); EC 4.2.1.1 (CA9 protein, human); EC 4.2.1.1 (Carbonic Anhydrase IX); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase XII)
[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:171204
[St] Status:MEDLINE



página 1 de 721 ir para página                         
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde