RESUMO
Acyclic glycosidopyrroles of type 1, synthesized in good overall yields, were evaluated for anti-viral activity. Compound 10i was found to inhibit the HIV-1 replication at concentrations that were very close to those cytotoxic for MT-4 cells. Compounds 10a,f,i inhibited both strains HSV-1 and HSV-2 at concentrations slightly below those cytotoxic for Vero cells. However for this series of glycosidopyrroles some relationship between calculated log P values and the observed cytotoxicity was found.
Assuntos
Antivirais/síntese química , Pirróis/síntese química , Animais , Antivirais/farmacologia , Chlorocebus aethiops , Pirróis/farmacologia , Células VeroRESUMO
A series of novel 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole derivatives was prepared and tested to evaluate their antimycotic, antibacterial and anti-HIV-1 activities. The reaction of thiocarbohydrazide with carboxylic acids at the melting temperature allows an improved preparation of the 5-substituted 4-amino-3-mercapto-1,2,4-triazole heterocycles which in turn allows an easier preparation of the 1,2,4-triazolo[3,4-b] [1,3,4]thiadiazole ring system. All tested compounds didn't show any significant activity.
Assuntos
Anti-Infecciosos/síntese química , Antivirais/síntese química , Tiadiazóis/síntese química , Fármacos Anti-HIV/síntese química , Fármacos Anti-HIV/farmacologia , Anti-Infecciosos/farmacologia , Antivirais/farmacologia , Linhagem Celular , Avaliação de Medicamentos , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Tiadiazóis/farmacologiaRESUMO
The series of 1-(1,3-dihydroxy-2-propoxy)methylpyrroles 2a-o were prepared in good overall yields according to Scheme I. When evaluated for antiviral activity against HIV-1, only compounds of the triphenyl series (R3 = NH2, N3, Br) were found to inhibit the HIV-1 replication at concentrations that were very not cytotoxic for MT-4 cells, with selectivity index 1.5-9.3. None of these compounds showed antibacterial or antifungal activity.
