RESUMO
In this work, a number of lipidic amino alcohols wereas synthesized and evaluated in vitro on cultures of Leishmania amazonensis and Leishmania chagasi. Nine amino alcohols showed inhibition of L. chagasi growth, and seven of them showed inhibition of L. amazonensis with IC(50) below 10 microm. Compound 11f was more active than the reference drug amphotericin B against L. chagasi promastigote forms.
Assuntos
Amino Álcoois/síntese química , Leishmania/efeitos dos fármacos , Tripanossomicidas/síntese química , Amino Álcoois/química , Amino Álcoois/farmacologia , Anfotericina B/farmacologia , Humanos , Leishmania/crescimento & desenvolvimento , Tripanossomicidas/química , Tripanossomicidas/farmacologiaRESUMO
A series of diamines and amino alcohols derived from 1-dodecanol, 1-tetradecanol, 1,2-dodecanediol and 1,2-tetradecanediol were synthesized and tested for their antitubercular activity. Compounds 3, 8 and 9 were found to be the most active (MIC of 6.25 microg/mL). Nine other compounds displayed activity against Mycobacterium tuberculosis, with a MIC of 12.5 microg/mL.
Assuntos
Amino Álcoois/farmacologia , Antituberculosos/farmacologia , Diaminas/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Amino Álcoois/síntese química , Antituberculosos/química , Diaminas/síntese química , Testes de Sensibilidade MicrobianaRESUMO
A series of diamines and amino alcohols derived from 1-dodecanol, 1-tetradecanol, 1,2-dodecanediol and 1,2-tetradecanediol were synthesized and tested for their antitubercular activity. Compounds 3, 8 and 9 were found to be the most active (MIC of 6.25 µg/mL). Nine other compounds displayed activity against Mycobacterium tuberculosis, with a MIC of 12.5 µg/mL.
Assuntos
Amino Álcoois/farmacologia , Antituberculosos/farmacologia , Diaminas/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Amino Álcoois/síntese química , Antituberculosos/química , Diaminas/síntese química , Testes de Sensibilidade MicrobianaRESUMO
A series of N- and C-alkylated amino alcohols and of their protected galactopyranosyl derivatives was synthesized and evaluated for antitubercular activity. Five of these compounds displayed good activity, with a MIC below 12.5mug/mL. The presence of the carbohydrate slightly affected the antibacterial activity.