RESUMO
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 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.
Assuntos
Amino Álcoois/síntese química , Amino Álcoois/farmacologia , Antituberculosos/síntese química , Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Alquilação , Amino Álcoois/química , Antituberculosos/química , Proliferação de Células , Células Cultivadas , Glicosilação , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
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
This work reports the preparation of several amino alcohols condensed with d-arabinose, d-glucose, and d-galactose derivatives. These compounds were evaluated in vitro for their cytotoxicity and ability to decrease nitric oxide production in J774A.1 cells. Arabinofuranoside derivatives 5a, 5b and 5c showed a significant inhibition of nitric oxide production (>80% at 5 µg/mL), while the galactopyranoside derivative 8d showed a notable nitric oxide inhibitory activity (126% at 0.5 µg/mL).
Assuntos
Amino Álcoois/química , Carboidratos/química , Óxido Nítrico/metabolismo , Amino Álcoois/síntese química , Amino Álcoois/toxicidade , Animais , Arabinose/química , Linhagem Celular Tumoral , Galactose/química , Glucose/química , Interferon gama/farmacologia , Lipopolissacarídeos/farmacologia , CamundongosRESUMO
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 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.