Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase
摘要:
The synthesis and inhibitory potencies of a novel series of beta-amino alcohols, based on the hit-compound 3-[3`-(4 ''-cyclopent-2```-en-1```-ylphenoxy)-2`-hydroxypropyl]-5,5 dimethylimidazolidine-2,4-dione as specific inhibitors of mycobacterial N-acetyltransferase (NAT) enzymes are reported. Effects of synthesised compounds on growth of Mycobacterium tuberculosis have been determined. (c) 2010 Elsevier Ltd. All rights reserved.
Silica Sulfuric Acid (SSA) as a Highly Efficient Heterogeneous Catalyst for Persilylation of Purine and Pyrimidine Nucleobases and Other <i>N</i>-Heterocycles Using Hmds
Purine and pyrimidine nucleobases and other N-heterocycles have been silylated with HMDS in excellent yields in the presence of a catalytic amount of silica sulfuric acid (SSA) as a heterogeneous catalyst. SSA utilizes a shorter reaction time and higher yields of silylated nucleobases. SSA is reusable for several times without a decrease in reactivity or yield of silylated adducts.
Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase
作者:Elizabeth Fullam、Areej Abuhammad、David L. Wilson、Matthew C. Anderton、Steve G. Davies、Angela J. Russell、Edith Sim
DOI:10.1016/j.bmcl.2010.12.099
日期:2011.2
The synthesis and inhibitory potencies of a novel series of beta-amino alcohols, based on the hit-compound 3-[3`-(4 ''-cyclopent-2```-en-1```-ylphenoxy)-2`-hydroxypropyl]-5,5 dimethylimidazolidine-2,4-dione as specific inhibitors of mycobacterial N-acetyltransferase (NAT) enzymes are reported. Effects of synthesised compounds on growth of Mycobacterium tuberculosis have been determined. (c) 2010 Elsevier Ltd. All rights reserved.