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  1 / 3990 MEDLINE  
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[PMID]:29289880
[Au] Autor:Ansari MF; Idrees D; Hassan MI; Ahmad K; Avecilla F; Azam A
[Ad] Endereço:Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025, New Delhi, India.
[Ti] Título:Design, synthesis and biological evaluation of novel pyridine-thiazolidinone derivatives as anticancer agents: Targeting human carbonic anhydrase IX.
[So] Source:Eur J Med Chem;144:544-556, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In order to obtain novel Human carbonic anhydrase IX (CAIX) inhibitors, a series of pyridine-thiazolidinone derivatives was synthesized and characterized by various spectroscopic techniques. The binding affinity of the compounds was measured by fluorescence binding studies and enzyme inhibition activity using esterase assay of CAIX. It was observed that compound 8 and 11 significantly inhibit the CAIX activity with the IC value, 1.61 µM and 1.84 µM, respectively. The binding-affinity of compound 8 and 11 for CAIX was significantly high with their K values 11.21 µM and 2.32 µM, respectively. Docking studies revealed that compound 8 and 11 efficiently binds in the active site cavity of CA IX by forming sufficient numbers of H-bonds and van der Waals interactions with active side residues. All the compounds were further screened in vitro for anticancer activity and found that compound 8 and 11 exhibit considerable anticancer activity against MCF-7 and HepG-2 cell lines. All these findings suggest that compound 8 and 11 may be further exploited as a novel pharmacophore model for the development of anticancer agents.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Anidrase Carbônica IX/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Desenho de Drogas
Piridinas/farmacologia
Tiazolidinas/farmacologia
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/metabolismo
Antineoplásicos/síntese química
Antineoplásicos/química
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica II/metabolismo
Anidrase Carbônica IX/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Piridinas/síntese química
Piridinas/química
Relação Estrutura-Atividade
Tiazolidinas/síntese química
Tiazolidinas/química
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Antineoplastic Agents); 0 (Carbonic Anhydrase Inhibitors); 0 (Pyridines); 0 (Thiazolidines); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.1 (CA9 protein, human); EC 4.2.1.1 (Carbonic Anhydrase IX); NH9L3PP67S (pyridine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180101
[St] Status:MEDLINE


  2 / 3990 MEDLINE  
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[PMID]:29226716
[Au] Autor:Hári-Kovács A; Soós J; Gyetvai T; Facskó A; Végh M
[Ad] Endereço:Szemészeti Klinika, Szegedi Tudományegyetem, Általános Orvostudományi Kar Szeged, Korányi fasor 10-11., 6720.
[Ti] Título:[Case report on choroidal effusion after oral acetazolamide administration: an unusual manifestation of a well-known idiosyncratic effect?]
[Ti] Título:Acetazolamid orális alkalmazása mellett jelentkezo chorioidealeválás két esete: ismert idioszinkráziás hatás szokatlan megjelenési formája?.
[So] Source:Orv Hetil;158(50):1998-2002, 2017 Dec.
[Is] ISSN:0030-6002
[Cp] País de publicação:Hungary
[La] Idioma:hun
[Ab] Resumo:Sulpha drugs are widely employed in medicine for various diseases and disorders. During the last several decades, numerous papers had been published on supra ciliary and posterior choroidal effusion likely presenting as an idiosyncratic effect of these drugs especially of acetazolamide. In each publication, the effusion was associated with either an acute angle-closure glaucoma or transitory myopia or both of these as leading symptoms. In the current publication, authors report on two cases where the acetazolamide-induced choroidal effusion was an accidental finding without either a myopic shift in refraction or an acute elevation in intraocular pressure. To our best knowledge, ours is the first report in the literature describing this unusual, "silent" form of a sulpha drug-induced choroidal effusion. Since the choroidal involvement may vary in size and location, and is not necessarily associated with acute glaucoma and myopia, one can assume that a considerable amount of acetazolamide-related ocular side-effects will not be discovered. The above case report aims to draw the attention of other specialities to the need for ophthalmic examination for their patients taking sulpha drugs with acute visual deterioration. Orv Hetil. 2017; 158(50): 1998-2002.
[Mh] Termos MeSH primário: Acetazolamida/efeitos adversos
Inibidores da Anidrase Carbônica/efeitos adversos
Doenças da Coroide/induzido quimicamente
[Mh] Termos MeSH secundário: Acetazolamida/administração & dosagem
Doença Aguda
Idoso de 80 Anos ou mais
Inibidores da Anidrase Carbônica/administração & dosagem
Doenças da Coroide/diagnóstico
Corpo Ciliar/patologia
Edema/induzido quimicamente
Seres Humanos
Masculino
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); O3FX965V0I (Acetazolamide)
[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:171212
[St] Status:MEDLINE
[do] DOI:10.1556/650.2017.30944


  3 / 3990 MEDLINE  
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[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 / 3990 MEDLINE  
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[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 / 3990 MEDLINE  
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[PMID]:27775976
[Au] Autor:Grey KR; Warshaw EM
[Ad] Endereço:From the *University of Minnesota Medical School; †HCMC Parkside Occupational and Contact Dermatitis Clinic; ‡Department of Dermatology, Minneapolis Veterans Affairs Medical Center; and §Department of Dermatology, University of Minnesota Medical School, Minneapolis.
[Ti] Título:Allergic Contact Dermatitis to Ophthalmic Medications: Relevant Allergens and Alternative Testing Methods.
[So] Source:Dermatitis;27(6):333-347, 2016 Nov/Dec.
[Is] ISSN:2162-5220
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Allergic contact dermatitis is an important cause of periorbital dermatitis. Topical ophthalmic agents are relevant sensitizers. Contact dermatitis to ophthalmic medications can be challenging to diagnose and manage given the numerous possible offending agents, including both active and inactive ingredients. Furthermore, a substantial body of literature reports false-negative patch test results to ophthalmic agents. Subsequently, numerous alternative testing methods have been described. This review outlines the periorbital manifestations, causative agents, and alternative testing methods of allergic contact dermatitis to ophthalmic medications.
[Mh] Termos MeSH primário: Dermatite Alérgica de Contato/etiologia
Dermatoses Faciais/etiologia
Lubrificantes Oftálmicos/efeitos adversos
Soluções Oftálmicas/efeitos adversos
[Mh] Termos MeSH secundário: Administração Oftálmica
Agonistas de Receptores Adrenérgicos alfa 1/efeitos adversos
Antagonistas Adrenérgicos beta/efeitos adversos
Antibacterianos/efeitos adversos
Anti-Infecciosos Locais/efeitos adversos
Anti-Inflamatórios/efeitos adversos
Antineoplásicos/efeitos adversos
Antivirais/efeitos adversos
Inibidores da Anidrase Carbônica/efeitos adversos
Antagonistas Colinérgicos/efeitos adversos
Glaucoma/tratamento farmacológico
Antagonistas dos Receptores Histamínicos/efeitos adversos
Seres Humanos
Agonistas Muscarínicos/efeitos adversos
Antagonistas Muscarínicos/efeitos adversos
Prostaglandinas Sintéticas/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Agonists); 0 (Adrenergic beta-Antagonists); 0 (Anti-Bacterial Agents); 0 (Anti-Infective Agents, Local); 0 (Anti-Inflammatory Agents); 0 (Antineoplastic Agents); 0 (Antiviral Agents); 0 (Carbonic Anhydrase Inhibitors); 0 (Cholinergic Antagonists); 0 (Histamine Antagonists); 0 (Lubricant Eye Drops); 0 (Muscarinic Agonists); 0 (Muscarinic Antagonists); 0 (Ophthalmic Solutions); 0 (Prostaglandins, Synthetic)
[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:161025
[St] Status:MEDLINE


  6 / 3990 MEDLINE  
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[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


  7 / 3990 MEDLINE  
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[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


  8 / 3990 MEDLINE  
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[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


  9 / 3990 MEDLINE  
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[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


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[PMID]:29271264
[Au] Autor:Monti SM; Meccariello A; Ceruso M; Szafranski K; Slawinski J; Supuran CT
[Ad] Endereço:a Institute of Biostructures and Bioimaging , Naples , Italy.
[Ti] Título:Inhibition studies of Brucella suis ß-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides.
[So] Source:J Enzyme Inhib Med Chem;33(1):255-259, 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) from the pathogenic bacterium Brucella suis, BsuCA1 and BsuCA2, were investigated for their inhibition profile with a series of pyridine-3-sulphonamide derivatives incorporating 4-hetaryl moieties. BsuCA1 was effectively inhibited by these sulphonamides with inhibition constants ranging between 34 and 624 nM. BsuCA2 was less sensitive to these inhibitors, with K s in the range of 62 nM - > 10 µM. The nature of the 4-substituent present on the pyridine ring was the main factor influencing the inhibitory profile against both isoforms, with 4-halogenophenylpiperazin-1-yl and 3,4,5-trisubstituted-pyrazol-1-yl derivatives showing the most effective inhibition. Some of these sulphonamides were most effective bacterial CA than human (h) CA I and II inhibitors, making them selective for the prokaryotic enzymes. Investigation of bacterial CA inhibitors may be relevant for finding antibiotics with a new mechanism of action compared to the clinically used agents for which substantial drug resistance emerged.
[Mh] Termos MeSH primário: Brucella suis/enzimologia
Inibidores da Anidrase Carbônica/química
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Piridinas/farmacologia
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Inibidores da Anidrase Carbônica/síntese química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Piridinas/síntese química
Piridinas/química
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Pyridines); 0 (Sulfonamides); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171229
[Lr] Data última revisão:
171229
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171223
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1413097



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