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Synthesis and Antimycobacterial Activity of Novel Amino Alcohols Containing Central Core of the Anti‐HIV Drugs Lopinavir and Ritonavir
Author(s) -
Gomes Claudia R. B.,
Moreth Marcele,
Cardinot Danielle,
Kopke Valquiria,
Cunico Wilson,
da Silva Lourenço Maria Cristina,
de Souza Marcus V. N.
Publication year - 2011
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01244.x
Subject(s) - lopinavir , ethambutol , ritonavir , minimum inhibitory concentration , chemistry , antimycobacterial , isoniazid , mycobacterium tuberculosis , human immunodeficiency virus (hiv) , pharmacology , stereochemistry , antibiotics , tuberculosis , rifampicin , biochemistry , medicine , virology , viral load , pathology , antiretroviral therapy
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 tuberculosi s H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in μ m . Ten amino alcohols evaluated displayed significant activity (MIC between 6.15 and 108.4 μ m ) when compared to first‐line drug ethambutol (MIC = 15.9 μ m ). Three of them showed more activity than ethambutol (MIC = 6.15; 6.21 and 13.4 μ m ). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti‐TB compounds.