关于无环嘧啶作为分枝杆菌抑制剂的研究。

Studies on acyclic pyrimidines as inhibitors of mycobacteria.

作者信息

Srivastav Naveen C, Manning Tracey, Kunimoto Dennis Y, Kumar Rakesh

机构信息

Department of Laboratory Medicine and Pathology, 1-41 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7.

出版信息

Bioorg Med Chem. 2007 Mar 1;15(5):2045-53. doi: 10.1016/j.bmc.2006.12.032. Epub 2006 Dec 23.

DOI:10.1016/j.bmc.2006.12.032

PMID:17218105

Abstract

In vitro anti-mycobacterial activities of several 5-substituted acyclic pyrimidine nucleosides containing 1-(2-hydroxyethoxy)methyl and 1-[(2-hydroxy-1-(hydroxymethyl) ethoxy)methyl] acyclic moieties are investigated against three mycobacteria viz. Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium, which cause serious infections and mortality in healthy people as well as patients with AIDS. 1-(2-Hydroxyethoxy)methyl-5-(1-azido-2-haloethyl or 1-azidovinyl) analogs (4-7), 1-[(2-hydroxy-1-(hydroxymethyl)ethoxy)methyl]-5-decynyluracil (37), and 1-[(2-hydroxy-1-(hydroxymethyl)ethoxy)methyl]-5-dodecynyluracil (38) exhibited significant in vitro anti-tubercular activity against these mycobacteria.

摘要

研究了几种含有1-(2-羟基乙氧基)甲基和1-[(2-羟基-1-(羟甲基)乙氧基)甲基]无环部分的5-取代无环嘧啶核苷对三种分枝杆菌，即结核分枝杆菌、牛分枝杆菌和鸟分枝杆菌的体外抗分枝杆菌活性，这些分枝杆菌会在健康人群以及艾滋病患者中引起严重感染和死亡。1-(2-羟基乙氧基)甲基-5-(1-叠氮基-2-卤代乙基或1-叠氮基乙烯基)类似物(4-7)、1-[(2-羟基-1-(羟甲基)乙氧基)甲基]-5-癸炔基尿嘧啶(37)和1-[(2-羟基-1-(羟甲基)乙氧基)甲基]-5-十二炔基尿嘧啶(38)对这些分枝杆菌表现出显著的体外抗结核活性。