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1.
Comb Chem High Throughput Screen ; 24(2): 220-232, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32646352

RESUMO

BACKGROUND: Several compounds have been synthesized as a therapeutic alternative for heart failure; however, its preparation requires special conditions. OBJECTIVE: The aim of this study, was to synthesize some aniline derivatives (4-9) from 3- ethynylaniline to evaluate their biological activity against heart failure. METHODS: The synthesis of aniline derivatives involved a series of reactions such as etherification, addition, and cyclization. The structure of all compounds obtained was confirmed by spectroscopic and spectrometric methods. In addition, to evaluate the biological activity of compounds, an ischemia/reperfusion injury model was used. RESULTS: The results showed that compound 8 decreases heart failure, which translates into a decrease in the infarction area compared to compounds 4-7 and 9. CONCLUSION: This study reports a facile method for the preparation of aniline derivatives. This method offers some advantages such as; a simple procedure, low cost, and easy work up. In addition, compound 8 showed an interesting biological activity against heart failure. This phenomenon is particularly interesting because the biological activity induced by this compound could involve a molecular mechanism that is different from other drugs used for the treatment of heart failure.


Assuntos
Compostos de Anilina/uso terapêutico , Desenho de Fármacos , Insuficiência Cardíaca/tratamento farmacológico , Compostos de Anilina/síntese química , Compostos de Anilina/química , Animais , Masculino , Estrutura Molecular , Ratos , Ratos Wistar
2.
Steroids ; 163: 108715, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32853676

RESUMO

Several studies have been reported for the preparation of hexacyclic-steroid derivatives; however, some reagents are expensive and require special conditions for handling. In this way, the objective of this study was to synthesize a hexacyclic-steroid derivative from 4-hydroxyestrone. The chemical structure was evaluated through both 1H NMR and 13C NMR spectroscopic analysis. The results showed good performance of the hexacyclic-steroid derivative. In conclusion in this study, an easy method for the preparation of the hexacyclic-steroid derivative is reported.


Assuntos
Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/síntese química , Hidroxiestronas/química , Técnicas de Química Sintética
3.
Steroids ; 160: 108654, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32439408

RESUMO

There are several reports for the preparation of furan derivatives using some protocols which requires special conditions. In this way, the aim of this study was to synthesize a new furan-steroid-propanone derivative from both 17α-ethynylestradiol and 2-nitro-17α-ethynylestradiol using some series of reactions such as aldolization, 2 + 2 addition and etherification. The chemical structure was evaluated through both 1H NMR and 13C NMR spectroscopic analysis. The results showed a good yielding from furan-steroid derivative. In conclusion, this investigation provides a facile synthesis of a new furan-steroid-propanone derivative, using some reagents which are not expensive and do not require special conditions for handling.


Assuntos
Técnicas de Química Sintética , Furanos/química , Propano/análogos & derivados , Propano/química , Esteroides/química , Desenho de Fármacos , Estrutura Molecular
4.
Steroids ; 158: 108620, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32119871

RESUMO

Several drugs have been prepared to treat of heart failure using some protocols which require dangerous reagents and specific conditions. The aim of this study was to synthesize a series of steroid derivatives (compounds 2 to 18) using some chemical strategies. The biological activity of steroid derivatives against heart failure was evaluated using an ischemia/reperfusion model. In addition, the effect exerted by compounds 4 or 5 on left ventricular pressure was evaluated in the absence or presence of yohimbine, butaxamine and methoctramine. The results showed that 1) both compounds 4 or 5 significantly decrease the heart failure (translated as infarct area) compared with the compounds 2, 3 and 6-18. In addition, the compound 4 and 5 decreased the left ventricular pressure in a dose-dependent manner and this effect was significantly inhibited in the presence of methoctramine (p = 005). In conclusion, the compounds 4 or 5 decrease both the infarct area and left ventricular pressure via M2-muscarinic receptor activation.


Assuntos
Desenho de Fármacos , Insuficiência Cardíaca/tratamento farmacológico , Receptor Muscarínico M2/agonistas , Receptor Muscarínico M2/metabolismo , Esteroides/farmacologia , Animais , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Insuficiência Cardíaca/metabolismo , Masculino , Conformação Molecular , Ratos , Ratos Wistar , Esteroides/síntese química , Esteroides/química , Relação Estrutura-Atividade
5.
Artigo em Inglês | MEDLINE | ID: mdl-31580254

RESUMO

BACKGROUND: There is some experimental data on the effect exerted by some steroid derivatives against ischemia/reperfusion injury; however, the molecular mechanism is very confusing, perhaps this phenomenon could be due to the protocols used and/or differences in the chemical structure of each one of the steroid derivatives. OBJECTIVES: The aim of this study was to synthesize a new bis-steroid-methanocyclobutanaphthalene- dione derivative using some tools chemical. METHODOLOGY: The biological activity exerted by the bis-steroid-methanocyclobutanaphthalene- dione derivative against ischemia/reperfusion injury was evaluated in an isolated heart model using noradrenaline, milrinone, dobutamine, levosimendan, and Bay-K- 8644 as controls. In addition, other alternative experiments were carried out to evaluate the biological activity induced by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure in the absence or presence of nifedipine. RESULTS: The results showed that 1) the bis-steroid-methanocyclobuta-naphthalene-dione derivative significantly decreases the ischemia-reperfusion injury translated as a decrease in the the infarct area in a similar manner to levosimendan drug; 2) both bis-steroidmethanocyclobuta- naphthalene-dione and Bay-K-8644 increase the left ventricular pressure and 3) the biological activity exerted by bis-steroid-methanocyclobuta-naphthalenedione derivative against left ventricular pressure is inhibited by nifedipine. CONCLUSION: In conclusion, the bis-steroid-methanocyclobuta-naphthalene-dione derivative decreases the area of infarction and increases left ventricle pressure via calcium channels activation; this phenomenon could constitute a new therapy for ischemia/reperfusion injury.


Assuntos
Agonistas dos Canais de Cálcio/farmacologia , Cardiotônicos/farmacologia , Traumatismo por Reperfusão Miocárdica/fisiopatologia , Naftoquinonas/farmacologia , Animais , Agonistas dos Canais de Cálcio/química , Cardiotônicos/química , Masculino , Traumatismo por Reperfusão Miocárdica/tratamento farmacológico , Naftoquinonas/química , Ratos Wistar , Função Ventricular Esquerda/efeitos dos fármacos , Pressão Ventricular/efeitos dos fármacos
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