Synthesis and antimycobacterial activity of novel amino alcohols containing central core of the anti-HIV drugs lopinavir and ritonavir.

Eleven new amino alcohol derivatives have been synthesized from reactions of lopinavir intermediate and heteroaromatic aldehyde in good yields. These compounds, the antiretrovirals (lopinavir and ritonavir) and lopinavir key intermediate 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. Ten amino alcohols evaluated displayed significant activity (MIC between 6.15 and 108.4 µM) when compared to first-line drug ethambutol (MIC = 15.9 µM). Three of them showed more activity than ethambutol (MIC = 6.15; 6.21 and 13.4 µM). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds.

Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives.

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.