Synthesis and antimycobacterial activities of glycosylated amino alcohols and amines

被引:38
作者
Katiyar, D
Tiwari, VK
Tewari, N
Verma, SS
Sinha, S
Gaikwad, A
Srivastava, A
Chaturvedi, V
Srivastava, R
Srivastava, BS
Tripathi, RP [1 ]
机构
[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India
[3] Cent Drug Res Inst, Div Microbiol, Lucknow 226001, Uttar Pradesh, India
关键词
tuberculosis; glycosyl amines; glycosyl amino alcohols; reductive amination; MDR tuberculosis;
D O I
10.1016/j.ejmech.2004.12.002
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Reduction of glycosyl P-amino esters (6-14 and 25-30) with lithium aluminum hydride resulted in glycosyl amino alcohols (15-23 and 31-36) in good yields. However, reductive amination of glycosyl aldehydes (1-3) with different amines in presence of sodium borohydride resulted in good to moderate yields of glycosyl amines (37-41). All the compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis H37Ra and H(37)Rv. Compounds 18, 21, 35 and 36 exhibited antitubercular activities with MIC ranging from 6.25 to 3.12 mu g ml(-1.) (c) 2005 Elsevier SAS. All rights reserved.
引用
收藏
页码:351 / 360
页数:10
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