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1.
Acta Pol Pharm ; 72(3): 497-506, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26642658

RESUMO

The present study was designed to investigate the effects of the extract of green tea and/or ginger on some hematological and immunobiochemical profiles in alloxan-induced diabetic rabbits. The results revealed that treatment of diabetic animals with extract of green tea and/or ginger elevated the decreased HDL-c and LDL-c but significantly decreased triglycerides, the elevated glucose and GOT concentrations. The result also displayed a non-significant increase in the levels of CRP and fibrinogen. The experiment also revealed that the elevated MDA and GSH level fell down to the normal control group. The result also showed that after green tea and/or ginger extract treatment, the lowered RBC, WBC counts, PCV, percentage of neutrophils were increased and the elevated MCV, MCH, and MCHC of diabetic rabbits were decreased to normal levels. Thus, the overall results may indicate that green tea and/or ginger extracts have a significant hypoglycemic effect in diabetic rabbits. In addition, the extracts may be capable of improving hyperlipidemia, the impaired kidney function and hemogram in alloxan-induced diabetic rabbits.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Chá , Zingiber officinale , Aloxano , Animais , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/imunologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Coelhos
2.
Arch Pharm (Weinheim) ; 343(11-12): 657-63, 2010 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21110342

RESUMO

A series of (Z)-2-(substituted aryl)-N-(3-oxo-4-(substituted carbamothioyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl) hydrazine carboxamides (6a-r) was synthesized using 2-amino-5-nitrophenol as a starting material. All the synthesized compounds possessed two hydrogen-bonding domains and their effect on the activity was studied thereof. The anticonvulsant activity was assessed by the maximal electroshock test (MES), subcutaneous pentylenetetrazole test (scPTZ) and intraperitoneal thiosemicarbazide test (ipTSC). Compounds (6b, 6h, 6i, and 6p) were found to be the most potent of the series as they showed 83-100% protection in the MES test. They also displayed considerable activity in the chemically induced seizure tests. Most of the tested compounds were devoid of the neurotoxic and hepatotoxic effects.


Assuntos
Anticonvulsivantes/síntese química , Oxazinas/síntese química , Amidas , Animais , Anticonvulsivantes/toxicidade , Avaliação Pré-Clínica de Medicamentos , Ligação de Hidrogênio , Oxazinas/farmacologia , Oxazinas/toxicidade , Convulsões/tratamento farmacológico
3.
Acta Pol Pharm ; 67(3): 239-46, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20524425

RESUMO

Various N,N'-diaryl-1,3-thiazole-2,4-diamines (3a-w) were synthesized by a three steps process. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. All the synthesized compounds were tested against two bacterial strains and two fungal strains. Bacterial strains included Gram positive Staphylococcus aureus and Gram negativeve Escherichia coli and fungal strains included Monascus purpurea and Penicillium citrinum. Most of the compounds showed moderate to good antibacterial as well as antifungal activity.


Assuntos
Antibacterianos , Antifúngicos , Diaminas , Tiazóis , Antibacterianos/síntese química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Cromatografia em Camada Fina , Diaminas/síntese química , Diaminas/farmacologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Relação Dose-Resposta a Droga , Desenho de Fármacos , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazóis/farmacologia
4.
J Enzyme Inhib Med Chem ; 25(4): 485-91, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20233086

RESUMO

A series of 4-thiazolidinones bearing a sulfonamide group (4a-w) were prepared by cyclizing various 5-bromo-2-methoxy-N'-[(1E)-arylmethylene/arylethylidene]benzenesulfonohydrazides. All the compounds were characterized by IR, (1)H NMR, and elemental analysis. The compounds were tested for their anticonvulsant activity utilizing MES and scPTZ animal models. The majority of the compounds exhibited significant activity against both animal models; however, compounds 4c, 4m, and 4o displayed promising activity and could be considered as leads for further investigations.


Assuntos
Anticonvulsivantes/química , Convulsões/tratamento farmacológico , Sulfonamidas/farmacologia , Tiazolidinas/farmacologia , Animais , Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Modelos Animais de Doenças , Cetonas , Ratos , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química , Tiazolidinas/síntese química , Tiazolidinas/química
5.
Acta Pharm ; 59(4): 441-51, 2009 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-19919933

RESUMO

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.


Assuntos
Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Tiadiazóis/química , Tiadiazóis/farmacologia , Acetofenonas , Animais , Anticonvulsivantes/síntese química , Avaliação Pré-Clínica de Medicamentos , Camundongos , Convulsões/tratamento farmacológico , Tiadiazóis/síntese química
6.
Acta Pol Pharm ; 66(2): 161-7, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19719050

RESUMO

Several heteroaryl semicarbazones were prepared by the reaction of heteroaryl hydrazine carboxamide with aryl aldehydes or ketones. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing pentylenetetrazole-induced seizure (PTZ) and maximal electroshock seizure (MES) tests at 30, 100 and 300 mg/kg dose levels. Neurotoxicity of the compounds was also assessed at the same dose levels. Three compounds of the series, 6d, 6i and 6n, exhibited significant anticonvulsant activity at 30 mg/kg dose level comparable to the standard drug, phenytoin.


Assuntos
Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Cumarínicos/síntese química , Cumarínicos/farmacologia , Semicarbazonas/síntese química , Semicarbazonas/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Animais , Anticonvulsivantes/toxicidade , Convulsivantes , Cumarínicos/toxicidade , Eletrochoque , Feminino , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Síndromes Neurotóxicas/psicologia , Pentilenotetrazol , Convulsões/induzido quimicamente , Convulsões/prevenção & controle , Semicarbazonas/toxicidade , Canais de Sódio/efeitos dos fármacos , Espectrofotometria Infravermelho , Tiazóis/toxicidade
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