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1.
Environ Pollut ; 308: 119608, 2022 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-35697139

RESUMO

Nowadays, microplastics represent emergent pollutants in terrestrial ecosystems that exert impacts on soil properties, affecting key soil ecological functions. In agroecosystems, plastic mulching is one of the main sources of plastic residues in soils. The present research aimed to evaluate the effects of two types of plastic sheets (un-biodegradable and biodegradable) on soil abiotic (pH, water content, concentrations of organic and total carbon, and total nitrogen) and biotic (respiration, and activities of hydrolase, dehydrogenase, ß-glucosidase and urease) properties, and on phytotoxicity (germination index of Sorghum saccharatum L. and Lepidium sativum L.). Results revealed that soil properties were mostly affected by exposure time to plastics rather than the kind (un-biodegradable and biodegradable) of plastics. After six months since mesocosm setting up, the presence of un-biodegradable plastic sheets significantly decreased soil pH, respiration and dehydrogenase activity and increased total and organic carbon concentrations, and toxicity highlighted by S. saccharatum L. Instead, the presence of biodegradable plastic sheets significantly decreased dehydrogenase activity and increased organic carbon concentrations. An overall temporal improvement of the investigated properties in soils covered by biodegradable plastic sheets occurred.


Assuntos
Plásticos Biodegradáveis , Poluentes do Solo , Agricultura , Carbono , Ecossistema , Oxirredutases , Plásticos , Solo/química , Poluentes do Solo/análise
2.
J Phys Condens Matter ; 21(12): 124201, 2009 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-21817443

RESUMO

Natural gadolinium is the strongest neutron-absorbing element and neutron diffraction studies of Gd-containing materials rely on the use of either enriched Gd isotopes or short neutron wavelengths where the absorption is weaker but, unfortunately, the neutron flux is also weak. We have employed a new sample-mounting technique to obtain neutron powder diffraction patterns from the intermetallic compound Gd(3)Ag(4)Sn(4) containing natural Gd, at a neutron wavelength of ∼ 2.37 Å where there is much greater flux. Here, we report the magnetic structure of Gd(3)Ag(4)Sn(4). The magnetic ordering temperature is 28.8(2) K. At 2.8 K the Gd(4e) sublattice is antiferromagnetically ordered along the crystal c-axis, commensurate with the crystal lattice. The Gd(2d) sublattice is also ordered along the c-axis but its magnetic structure is incommensurate with the crystal lattice.

3.
Bioorg Med Chem Lett ; 16(22): 5801-4, 2006 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-16982191

RESUMO

The synthesis of a new class of 9-(S)-dihydroerythromycin derivatives and their anti-inflammatory activity on in vivo PMA assay are described. Modifying the desosamine sugar on the C-3' amino group, it was possible to differentiate between anti-biotic and anti-inflammatory action. The compounds are completely devoid of anti-microbial effects but their anti-inflammatory properties are enhanced. These results strongly suggest the potential of macrolides as a new class of anti-inflammatory agents.


Assuntos
Amino Açúcares/química , Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Eritromicina/análogos & derivados , Eritromicina/uso terapêutico , Animais , Anti-Inflamatórios/síntese química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Desenho de Fármacos , Edema/patologia , Eritromicina/síntese química , Eritromicina/farmacologia , Camundongos
4.
Bioorg Med Chem Lett ; 11(1): 33-7, 2001 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-11140727

RESUMO

This communication describes the synthesis and in vitro evaluation of a novel and potent series of phosphodiesterase type IV (PDE4) inhibitors. The compounds described present substituents in position 4 of the phthalazine ring to replace the commonly observed cyclopentyloxy moiety of rolipram analogues. Preliminary evidences of reduced side effects compared to standards and improved pharmacokinetic properties for selected derivatives are also reported.


Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Ftalazinas/síntese química , Ftalazinas/farmacologia , 3',5'-AMP Cíclico Fosfodiesterases/metabolismo , Animais , Benzamidas/farmacologia , Disponibilidade Biológica , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Inibidores Enzimáticos/química , Cobaias , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Monócitos/efeitos dos fármacos , Monócitos/metabolismo , Neutrófilos/efeitos dos fármacos , Neutrófilos/enzimologia , Ftalazinas/química , Ligação Proteica , Piridinas/farmacologia , Rolipram/metabolismo , Fator de Necrose Tumoral alfa/biossíntese
5.
Bioorg Med Chem Lett ; 10(19): 2235-8, 2000 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-11012037

RESUMO

This communication describes the synthesis and in vitro evaluation of a novel and potent series of phosphodiesterase type IV (PDE4) inhibitors. The compounds described represent conformationally constrained analogues of RP 73401, Piclamilast. Preliminary evidences of reduced side effects of II compared to standards are also reported.


Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Inibidores de Fosfodiesterase/síntese química , Inibidores de Fosfodiesterase/farmacologia , Ftalazinas/síntese química , Ftalazinas/farmacologia , Benzamidas/química , Benzamidas/farmacologia , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Desenho de Fármacos , Humanos , Estrutura Molecular , Inibidores de Fosfodiesterase/química , Ftalazinas/química , Piridinas/química , Piridinas/farmacologia , Rolipram/química , Rolipram/farmacologia
6.
Farmaco ; 46(7-8): 887-97, 1991.
Artigo em Inglês | MEDLINE | ID: mdl-1793473

RESUMO

The synthesis of new 2-(3-bromo-5-isoxazolylideneamino-oxy)acetic acids and their condensation derivatives with suitable beta-lactam nuclei is reported. Their antibacterial properties have been tested in vitro. An interesting activity against Gram-positive bacteria including beta-lactamase-producing microorganisms was found among the cephalosporanic acid derivatives.


Assuntos
Antibacterianos/síntese química , Isoxazóis/síntese química , Antibacterianos/farmacologia , Cefalosporinas/síntese química , Cefalosporinas/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/enzimologia , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/enzimologia , Isoxazóis/farmacologia , Testes de Sensibilidade Microbiana , Penicilinas/síntese química , Penicilinas/farmacologia , beta-Lactamases/biossíntese , beta-Lactamas/síntese química , beta-Lactamas/farmacologia
7.
Farmaco ; 46(1): 21-31, 1991 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-2054039

RESUMO

The synthesis of 3-bromo-4,5,6,7-tetrahydro-1,2-benzoisoxazole derivatives and their activity against human pathogen fungi are reported. In particular, compound 3,5-dibromo-6,7-dihydro-1,2-benzoisoxazol-4-(5H)-one showed a broad antifungal spectrum and good fungicidal activity against Trichophyton mentagrophytes.


Assuntos
Antifúngicos/síntese química , Isoxazóis/síntese química , Animais , Antifúngicos/farmacologia , Antifúngicos/toxicidade , Fungos/efeitos dos fármacos , Técnicas In Vitro , Isoxazóis/farmacologia , Isoxazóis/toxicidade , Testes de Sensibilidade Microbiana , Testes de Mutagenicidade , Mutagênicos , Ratos , Salmonella typhimurium/efeitos dos fármacos
8.
Arzneimittelforschung ; 39(6): 642-6, 1989 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-2775328

RESUMO

A series of diazacycloalkane-quinazoline derivatives of isoxazoles were synthesized and tested in order to identify new potent and selective alpha 1-antagonists. A preliminary screening by using in vitro tests such as binding assay (3H-prazosin and 3H-rauwolscine displacement) and analysis of antagonistic activity in isolated rat aorta (norepinephrine-induced response) and in isolated rat vas deferens (clonidine-induced response) indicated that many of these compounds exhibited a good affinity and selectivity towards alpha 1-adrenergic receptors associated with potent pharmacological activity. In particular, a 3-bromo-5-isoxazolecarbonyl derivative, selected for further in vivo investigation, was provided with as high antihypertensive action as prazosin in spontaneously hypertensive rats (SHR) coupled to a shallow dose-response curve by oral route. Moreover, a higher ratio between oral antihypertensive doses in SHR and normotensive rats was found with respect to reference compound prazosin.


Assuntos
Anti-Hipertensivos , Isoxazóis/farmacologia , Oxazóis/farmacologia , Animais , Anti-Hipertensivos/síntese química , Aorta Torácica/efeitos dos fármacos , Ligação Competitiva/efeitos dos fármacos , Fenômenos Químicos , Química , Clonidina/farmacologia , Técnicas In Vitro , Isoxazóis/síntese química , Espectroscopia de Ressonância Magnética , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Norepinefrina/metabolismo , Prazosina/metabolismo , Ratos , Ratos Endogâmicos SHR , Ratos Endogâmicos , Ratos Endogâmicos WKY , Ducto Deferente/efeitos dos fármacos , Ioimbina/metabolismo
10.
J Antibiot (Tokyo) ; 40(11): 1555-62, 1987 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-3693126

RESUMO

The synthesis of new 2-(3-substituted-5-isoxazolyl)-2-methoxyiminoacetic acids and their condensation derivatives with a suitable cephalosporanic nucleus, is reported. Their antibacterial properties were tested in vivo and in vitro also against beta-lactamase producer microorganisms; particularly the oral bioavailability of some of these new derivatives was studied.


Assuntos
Antibacterianos , Cefalosporinas/síntese química , Isoxazóis/síntese química , Oxazóis/síntese química , Animais , Infecções Bacterianas/tratamento farmacológico , Disponibilidade Biológica , Cefalosporinas/análise , Cefalosporinas/uso terapêutico , Isomerismo , Isoxazóis/análise , Isoxazóis/uso terapêutico , Testes de Sensibilidade Microbiana , Ratos , Relação Estrutura-Atividade
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