Instituto de Tecnologia em Fármacos - Farmanguinhos, FioCruz - Fundação Oswaldo Cruz, R Sizenando Nabuco, 100 Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
Eur J Med Chem. 2011 Mar;46(3):974-8. doi: 10.1016/j.ejmech.2011.01.004. Epub 2011 Jan 13.
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.
从（2S,3S）Boc-苯丙氨酸环氧化物、胡椒基胺和芳基磺酰氯的反应中合成了 13 种新的羟乙基胺，产率良好。这些化合物被评估为抗结核分枝杆菌 H37Rv 的抗菌剂，使用阿尔玛蓝药敏试验，并以微摩尔（μM）为单位表示最小抑制浓度（MIC）。与一线药物乙胺丁醇（EMB）相比，两种氨基醇表现出显著的活性。因此，这类化合物可能是开发治疗结核病的新型先导化合物的良好起点。
