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1.
Acta Pol Pharm ; 69(1): 53-62, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22574507

RESUMO

A series of new 2-[(1-substituted phenylethylidine) hydrazine]-N-phenyl-1H-benzo[d]imidazole-1-carbothioamides (4a-n) were designed and synthesized to have the pharmacophoric elements essential for anticonvulsant activity. The key step in the synthesis of the title compounds involves the reaction of 2-mercaptobenzimidazole with hydrazine hydrate, substituted acetophenones and phenylisothiocyanate to get the compounds in good yields. All the newly synthesized compounds were screened by two most adopted models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Interestingly, compounds 4e, 4f, 4g, 4h and 4j exhibited potent anticonvulsant results and in the neurotoxicity screening, most of the compounds were devoid of toxicity at the dose of 60 and 100 mg/kg.


Assuntos
Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Desenho de Fármacos , Convulsões/prevenção & controle , Animais , Anticonvulsivantes/toxicidade , Benzimidazóis/toxicidade , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Estimulação Elétrica , Feminino , Masculino , Estrutura Molecular , Pentilenotetrazol , Ratos , Convulsões/etiologia , Relação Estrutura-Atividade
2.
Curr Top Med Chem ; 12(9): 1072-92, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22352863

RESUMO

The use of current antiepileptic drugs has been questioned due to the nonselectivity of the drugs and the undesirable side effects posed by them. This led to an intensive investigation in this area worldwide during the past 10 years. There have been some significant outcomes and the findings are promising as far as drug efficacy and safety is concerned. This review covers the new anticonvulsant agents that have shown encouraging activities and less neurotoxicity. A detailed pharmacology and pathophysiology of different types of epilepsy is described here with the structural classification of most active agents. The new structural classes of compounds may prove as lead molecules and good candidates for the future investigations.


Assuntos
Anticonvulsivantes/uso terapêutico , Epilepsia/tratamento farmacológico , Animais , Anticonvulsivantes/efeitos adversos , Anticonvulsivantes/química , Epilepsia/fisiopatologia , Humanos , Estrutura Molecular
3.
J Pharm Bioallied Sci ; 3(2): 194-212, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21687347

RESUMO

Depression is currently the fourth leading cause of disease or disability worldwide. Antidepressant is approved for the treatment of major depression (including paediatric depression), obsessive-compulsive disorder (in both adult and paediatric populations), bulimia nervosa, panic disorder and premenstrual dysphoric disorder. Antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. Many drugs produce an antidepressant effect, but restrictions on their use have caused controversy and off-label prescription a risk, despite claims of superior efficacy. Our current understanding of its pathogenesis is limited and existing treatments are inadequate, providing relief to only a subset of people suffering from depression. Reviews of literature suggest that heterocyclic moieties and their derivatives has proven success in treating depression.

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