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1.
Bioorg Med Chem Lett ; 22(17): 5639-47, 2012 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-22871579

RESUMO

Novel polysubstituted pyrroles have been designed and accessed via a one-pot multicomponent reaction followed by Pd-mediated C-C bond forming reactions. All the compounds synthesized were tested for their PDE4B inhibitory properties in vitro and two of them obtained via Heck reaction showed significant inhibition. The docking results suggested that these alkenyl derivatives containing ester moiety interact well with the PDE4B protein in silico where the ester carbonyl oxygen played a key role. The pyrrole framework presented here could be a new template for the identification of small molecule based novel inhibitors of PDE4. The single crystal X-ray data of a representative compound is presented.


Assuntos
Nucleotídeo Cíclico Fosfodiesterase do Tipo 4/metabolismo , Inibidores da Fosfodiesterase 4/química , Inibidores da Fosfodiesterase 4/farmacologia , Pirróis/química , Pirróis/farmacologia , Animais , Catálise , Linhagem Celular , Cristalografia por Raios X , Modelos Moleculares , Paládio/química , Relação Estrutura-Atividade
2.
Chemosphere ; 58(4): 507-14, 2005 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-15620742

RESUMO

Many sites in the industrial region of Kattedan near Hyderabad, Andhra Pradesh (AP), India are contaminated with high concentrations of lead. The use of plants to remove toxic metals from soils (phytoremediation) is emerging as a potential strategy for cost-effective and environmentally sound remediation of contaminated soils. We studied remediation of soils contaminated with lead using a lead hyperaccumulating plant, Hemidesmus indicus. The ability of this plant to accumulate lead in shoots and roots was studied with pot experiments. The results showed that accumulation was maximum in roots for the first 1-3 weeks and later for a contact period of three months, the accumulation rate was maximum in shoots. In addition we used various chelating agents such as EDTA, HEDTA, DTPA and CDTA to determine the best chemical modifier for efficient lead removal from contaminated soils. The effect on lead accumulation of plant in the presence of various metal co-ions was also studied. An attempt was made for the decontamination of lead from five different "Real-life" soils of Kattedan using H. indicus.


Assuntos
Hemidesmus/metabolismo , Chumbo/metabolismo , Poluentes do Solo/metabolismo , Solo/análise , Quelantes/química , Quelantes/farmacologia , Resíduos Industriais , Raízes de Plantas/química , Brotos de Planta/química , Poluentes do Solo/isolamento & purificação , Poluentes Químicos da Água/isolamento & purificação , Poluentes Químicos da Água/metabolismo
3.
J Hazard Mater ; 108(1-2): 111-7, 2004 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-15081169

RESUMO

Because of the severity of heavy metal contamination and potential adverse health impact on the public, a tremendous effort has taken place to purify waters containing toxic metal ions. Traditional methods which have been employed prove to be costly and prohibitive for low level waste remediation. Biosorption is presented as an alternative to traditional physicochemical means for removing toxic metals from ground and wastewaters. Most recently, plant based biomaterials have been of interest. The bark of Hemidesmus indicus, an extensively available plant biomass commonly called as Indian sarsaparilla was used as biomaterial for removal of lead from aqueous streams. Batch experiments were carried out with immobilized biomass of H. indicus (IPBFIX) to optimize the experimental parameters like effect of contact time, initial metal concentration, initial IPBFIX concentration and co-metal ion effect on biosorption of lead from contaminated waters. Column experiments were performed under flow conditions for regeneration and recycle efficiency of IPBFIX and was found to be effective for three cycles. Elution experiments were carried out to remove lead ions from loaded IPBFIX and 100% elution was achieved with a 0.1M HNO(3) solution. The effectiveness of the IPBFIX for biosorption of lead ions was demonstrated using the wastewater samples emanating from a non-ferrous metal industry and the results are presented in this paper. The results from these studies will be useful for a novel phytofiltration technology to remove and recover lead from wastewaters and this can also be well adapted for secondary treatment or polishing of wastewaters. An attempt has been made to remove lead from the lead polluted waters (both ground and surface) from an industrially contaminated sites.


Assuntos
Hemidesmus/química , Chumbo/isolamento & purificação , Casca de Planta/química , Poluentes da Água/isolamento & purificação , Purificação da Água/métodos , Adsorção , Biodegradação Ambiental , Biomassa , Resíduos Industriais , Íons , Eliminação de Resíduos Líquidos
4.
Environ Int ; 29(7): 1001-8, 2004 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-14592578

RESUMO

Kolleru lake is the largest fresh water lake in the districts of East and West Godavari of Andhra Pradesh, India. Many anthropogenic sources contribute to the heavy metal pollution in the lake and the bioaccumulation of heavy metals in fish helps in assessing the aquatic pollution. Total contents and fractionation of selected heavy metals, viz., Zn, Cu, Cd, Pb, Cr, Ni and Co were measured in sediment sample and three edible fish. The investigation aimed at revealing differences in the accumulation pattern of heavy metals in fish inhabiting sediments characterized by varying metal bioavailability. The metal concentrations were found to be greater than the background concentrations of sediments indicating the anthropogenic origin of metals. Good recovery values were obtained for metal contents in sediments and fish. Large fractions of Zn, Cd and Cu were associated with mobile fraction of sediment and showed greater bioaccumulation in fish whereas Ni and Co were least mobilisable. The results clearly indicate that the fish of Kolleru lake are contaminated with metals and not advisable for human consumption.


Assuntos
Contaminação de Alimentos , Metais Pesados/análise , Metais Pesados/farmacocinética , Poluentes da Água/análise , Poluentes da Água/farmacocinética , Animais , Disponibilidade Biológica , Sedimentos Geológicos/química , Humanos , Índia , Distribuição Tecidual
5.
Environ Int ; 29(5): 601-11, 2003 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-12742403

RESUMO

Different areas in the industrial region of Patancheru near Hyderabad, Andhra Pradesh (A.P), India are contaminated with high concentration of arsenic, which is attributed to industrial source like veterinary chemicals, pharmaceuticals, pesticide industries, etc. Fourteen villages of this area of Patancheru were assessed for arsenic contamination by collecting samples of water (surface and ground), soil, fodder, milk, and vegetables. The total arsenic content in the whole blood, urine, hair, and nails of the residents showing arsenical skin lesions and other clinical manifestations were also studied. To understand the bioavailability of arsenic in this environment and its possible entry into human food chain, speciation studies of arsenic was carried out and the results are presented in this paper.


Assuntos
Intoxicação por Arsênico , Arsênio/análise , Arsênio/farmacocinética , Contaminação de Alimentos , Poluentes do Solo/análise , Poluentes da Água/análise , Animais , Disponibilidade Biológica , Bovinos , Cadeia Alimentar , Cabelo/química , Humanos , Índia , Indústrias , Leite/química , Unhas/química , Saúde Pública , Medição de Risco , Distribuição Tecidual , Urina/química , Verduras
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