title: Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives.
abstract: 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.
authors.affiliation: Instituto de Tecnologia em Fármacos - Farmanguinhos, FioCruz - Fundação Oswaldo Cruz, R Sizenando Nabuco, 100 Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil. wjcunico@yahoo.com.br
authors.forename: Wilson
authors.initials: W
authors.lastname: Cunico
authors.forename: Claudia R B
authors.initials: CR
authors.lastname: Gomes
authors.forename: Maria L G
authors.initials: ML
authors.lastname: Ferreira
authors.forename: Thaís G
authors.initials: TG
authors.lastname: Ferreira
authors.forename: Danielle
authors.initials: D
authors.lastname: Cardinot
authors.forename: Marcus V N
authors.initials: MV
authors.lastname: de Souza
authors.forename: Maria C S
authors.initials: MC
authors.lastname: Lourenço
mesh_terms: D000605:Amino Alcohols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004977:Ethambutol / Q000031:analogs & derivatives; D006801:Humans; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy*
chemical_list: D000605:Amino Alcohols; D000995:Antitubercular Agents; D004977:Ethambutol