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1.
Bioorg Chem ; 117: 105418, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34736133

RESUMO

New sulfonylbiguanide hydrochloride salts and sulfonylurea derivatives containing two sulfonyl groups were synthesized through the reaction of arylsulfonohydrazides with cyanoguanidine and p-tolylsulfonylisocyanate, respectively. Oral treatment of hyperglycemic rats with the synthesized sulfonylbiguanide derivatives 2 and sulfonylurea derivatives 3 revealed that sulfonylurea derivatives 3a and 3c possessed significant decrease of the elevated glucose in compression with the anti-diabetic standard drugs. Effects of the synthesized sulfonylurea derivatives 3a and 3c on the diabetic properties towards α-amylase, liver function enzyme levels (AST, ALT, ALP, TB and γ-GT), kidney functions (urea and creatinine), lipids profiles (TG, TL, TC and HDL-C) were studied. Also, the effect of sulfonylurea derivatives 3a and 3c as antioxidants (reduced glutathione and lipid peroxide) was evaluated. Histopathological examination of hepatic and pancreatic tissues was investigated. The obtained results suggested that the most potent sulfonylurea derivatives 3a and 3c might be possible used as novel diabetic inhibitor agents.


Assuntos
Biguanidas/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Compostos de Sulfonilureia/uso terapêutico , Animais , Biguanidas/síntese química , Biguanidas/química , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/patologia , Relação Dose-Resposta a Droga , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Masculino , Estrutura Molecular , Ratos , Ratos Wistar , Estreptozocina , Relação Estrutura-Atividade , Compostos de Sulfonilureia/síntese química , Compostos de Sulfonilureia/química
2.
Bioorg Chem ; 92: 103290, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31561109

RESUMO

Series of new sulfonylurea derivatives (gliclazide analogues) was synthesized and characterized. Thus, p-tolylsulfonylisocyanate was left to react with different amino derivatives under mild conditions to afford the desired sulfonylurea derivatives 1-5. The molecular structure of the compound N-(2,6-Dichlorophenylcarbamoyl)-4-methylbenzenesulfonamide, 1c has been elucidated by single crystal X-ray diffraction. Anti-diabetic properties of the synthesized compounds relative to anti-diabetic drug (gliclazidem MR60) were carried out, where most of the tested compounds showed significant activity for reducing the blood glucose level. The results revealed that compounds 1c and 5 showed better anti-diabetic activities compared with gliclazide. Activity of the most potent derivatives of sulfonylurea compounds namely 1c and 5 were increased using coated nanostructure tetraethyl orthosilicate (TEOS) as a modified release (MR) agent. The effect of the prepared sulfonylurea compounds against the diabetic condition was investigated using specific selected biomarkers as of liver enzyme activities as transaminases (AST, ALT) and alkaline phosphatase (ALP), lipids profiles; total cholesterol (TC), triacylglycerols (TG) and total lipid (TL). The antioxidants, oxidative stress biomarkers and histological examination were also examined and discussed.


Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/farmacologia , Compostos de Sulfonilureia/farmacologia , Animais , Antioxidantes/síntese química , Antioxidantes/química , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/metabolismo , Relação Dose-Resposta a Droga , Glutationa/análise , Glutationa/metabolismo , Hiperglicemia/induzido quimicamente , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Malondialdeído/análise , Malondialdeído/metabolismo , Estrutura Molecular , Nanopartículas/química , Tamanho da Partícula , Ratos , Estreptozocina , Relação Estrutura-Atividade , Compostos de Sulfonilureia/síntese química , Compostos de Sulfonilureia/química , Propriedades de Superfície
3.
Arch Pharm (Weinheim) ; 350(11)2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29027251

RESUMO

New 1-arylamidebiguanide hydrochloride salts were synthesized via reaction of hydrazide derivatives with dicyandiamide in acidic medium. The structure of the obtained derivatives was characterized by spectroscopic and elemental analysis tools. The anti-diabetic properties of the synthesized compounds were determined. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives showed a significant decrease of the elevated glucose in comparison with the anti-diabetic standard drug, metformin. The effects of the synthesized biguanide derivatives on the diabetic properties regarding liver function enzyme activities (AST, ALT, and ALP), lipid profiles (TC, TG, and TL), lipid peroxide, and nitrous oxide as well as histopathological characteristics were investigated and discussed.


Assuntos
Biguanidas/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/farmacologia , Administração Oral , Animais , Biguanidas/síntese química , Biguanidas/química , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Insulina/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Testes de Função Hepática , Masculino , Metformina/farmacologia , Óxido Nitroso/metabolismo , Ratos
4.
Drug Res (Stuttg) ; 67(10): 557-563, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28651259

RESUMO

New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level. Additionally, anti-diabetic properties towards liver function enzyme activities (AST, ALT and ALP), lipids profiles (TC, TG and TL), lipid peroxide and nitrous oxide as well as histopathological studies relative to metformin hydrochloride were investigated and discussed.


Assuntos
Biguanidas/síntese química , Biguanidas/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/síntese química , Hipoglicemiantes/farmacologia , Lipídeos/sangue , Fígado/efeitos dos fármacos , Metformina/farmacologia , Metformina/uso terapêutico , Óxido Nitroso/química , Animais , Diabetes Mellitus Tipo 2/sangue , Resistência à Insulina , Ratos
5.
Eur J Med Chem ; 64: 111-20, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23644194

RESUMO

New series of thiourea derivatives incorporating a hippuric acid moiety have been synthesized through the reaction of 4-hippuric acid isothiocyanate with various nitrogen nucleophiles such as aliphatic amines, aromatic amines, sulfa drugs, aminopyrazoles, phenylhydrazine and hydrazides. The synthesized compounds were tested against bacterial and fungal strains. Most of compounds, such as 2-(4-(3-(3-bromophenyl)thioureido)benzamido)acetic acid and 2-(4-(3-(4-(N-pyrimidin-2-ylsulfamoyl)phenyl)thioureido)benzamido)acetic acid, showed significant antibacterial and antifungal activities. These compounds comprise a new class of promising broad-spectrum antibacterial and antifungal agents.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Hipuratos/farmacologia , Tioureia/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Hipuratos/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Tioureia/química
6.
Eur J Med Chem ; 45(8): 3365-73, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20510483

RESUMO

Novel 3-aryl-4(3H)-quinazolinone-2-carboxaldehydes, their corresponding Schiff's base and thiosemicarbazone derivatives were synthesized from the starting 5-iodo anthranilic acid. Copper(II), zinc(II) complexes of some thiosemicarbazone derivatives were also synthesized and characterized. Screening for some selected compounds was carried out to probe their potential anticonvulsant, analgesic, cytotoxic as well as their antimicrobial activities.


Assuntos
Compostos Organometálicos/síntese química , Compostos Organometálicos/farmacologia , Tiossemicarbazonas/síntese química , Tiossemicarbazonas/farmacologia , Analgésicos/síntese química , Analgésicos/química , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Anticonvulsivantes/síntese química , Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Bactérias/efeitos dos fármacos , Linhagem Celular Tumoral , Feminino , Fungos/efeitos dos fármacos , Dose Letal Mediana , Camundongos , Testes de Sensibilidade Microbiana , Compostos Organometálicos/química , Compostos Organometálicos/uso terapêutico , Pentilenotetrazol/farmacologia , Ratos , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Tiossemicarbazonas/química , Tiossemicarbazonas/uso terapêutico
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