Tripathi R P, Tiwari V K, Tewari N, Katiyar D, Saxena N, Sinha S, Gaikwad A, Srivastava A, Chaturvedi V, Manju Y K, Srivastava R, Srivastava B S
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem. 2005 Oct 1;13(19):5668-79. doi: 10.1016/j.bmc.2005.05.021.
Conjugate addition of diamines to glycosyl olefinic esters 1a and 1b followed by reduction of resulting bis-glycosyl beta-amino esters (2-7 and 14-19) with lithium aluminium hydride led to the respective glycosyl amino alcohols (8-13 and 20-25) in moderate to good yields. All the compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis H(37)Ra and H(37)Rv. Few of the compounds exhibited antitubercular activity with MIC as low as 6.25-3.12microg/mL in virulent and avirulent strains. Compound 13 was found to be active against MDR strain and showed mild protection in mice.
二胺与糖基烯酸酯1a和1b进行共轭加成，随后用氢化铝锂还原所得的双糖基β-氨基酯（2-7和14-19），以中等至良好的产率得到相应的糖基氨基醇（8-13和20-25）。对所有化合物针对结核分枝杆菌H(37)Ra和H(37)Rv的抗结核活性进行了评估。少数化合物在强毒株和无毒株中表现出抗结核活性，最低MIC为6.25-3.12微克/毫升。发现化合物13对耐多药菌株有活性，并在小鼠中显示出轻度保护作用。
