Details

Autor(en) / Beteiligte

• Cunico, Wilson
• Gomes, Claudia R.B.
• Ferreira, Maria L.G.
• Ferreira, Thaís G.
• Cardinot, Danielle
• de Souza, Marcus V.N.
• Lourenço, Maria C.S.

Titel

Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives

Ist Teil von

• European journal of medicinal chemistry, 2011-03, Vol.46 (3), p.974-978

Ort / Verlag

Kidlington: Elsevier Masson SAS

Erscheinungsjahr

2011

Quelle

MEDLINE

Beschreibungen/Notizen

• Thirteen new hydroxyethylamines have been synthesized from reactions of (2S,3S)Boc-phenylalanine epoxide, piperonylamine and arenesulfonyl chlorides in good yields. These compounds were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in μM. Two amino alcohols displayed significant activity when compared with first line drug ethambutol (EMB). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of tuberculosis. Thirteen amino alcohols have been synthesized from (2S,3S)Boc-phenylalanine epoxide, piperonylamine and arenesulfonyl chlorides in good yields. These compounds were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv. [Display omitted] ► Synthesis of ethambutol analogues. ► hydroxyethysulfonamides as antitubercular agents. ► the presence of amino alcohol is crucial for activity.