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1.
J Med Chem ; 32(2): 297-301, 1989 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-2913293

RESUMO

Some N-(dipeptidyl)-S-acetylcysteamine and N,N'-(dipeptidyl)cystamine salt derivatives were synthesized and evaluated as candidate radioprotector agents. Toxicity and radioprotective activity as the dose reduction factor (DRF) were determined in vivo on mice and compared to N-glycyl-S-acetylcysteamine trifluoroacetate. One of the most interesting compounds of this series was N-glycylglycyl-S-acetylcysteamine trifluoroacetate (8).


Assuntos
Cistamina/análogos & derivados , Cisteamina/análogos & derivados , Protetores contra Radiação/síntese química , Animais , Cistamina/síntese química , Cistamina/farmacologia , Cisteamina/síntese química , Cisteamina/farmacologia , Dipeptídeos/farmacologia , Camundongos , Protetores contra Radiação/farmacologia
2.
J Med Chem ; 29(11): 2217-25, 1986 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-3023610

RESUMO

A variety of N-(aminoalkanoyl)-S-acylcysteamine and N,N'-bis(aminoalkanoyl)cystamine salt derivatives were synthesized. Toxicity and radioprotective activity (as the dose reduction factor DRF) were determined in vivo on mice and compared to WR 2721 and S-acetylcysteamine hydrochloride. One of the most interesting compounds of this series was N-glycyl-S-acetylcysteamine trifluoroacetate (16, I 102). Structure-activity relationships are discussed.


Assuntos
Cistamina/análogos & derivados , Cisteamina/análogos & derivados , Protetores contra Radiação/síntese química , Amifostina/farmacologia , Animais , Cistamina/farmacologia , Cisteamina/farmacologia , Feminino , Masculino , Camundongos , Protetores contra Radiação/farmacologia , Relação Estrutura-Atividade
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