对硕大利什曼原虫有效的新型化合物。
Novel compounds active against Leishmania major.
作者信息
St George Stephanie, Bishop Jeanette V, Titus Richard G, Selitrennikoff Claude P
机构信息
MycoLogics, Inc., 12635 E. Montview Blvd., Suite 215, Aurora, CO 80010, USA.
出版信息
Antimicrob Agents Chemother. 2006 Feb;50(2):474-9. doi: 10.1128/AAC.50.2.474-479.2006.
Abstract
Leishmania major is an important trypanosomatid pathogen that causes leishmaniasis, which is a serious disease in much of the Old World. Current treatments include a small number of antimony compounds that, while somewhat effective, are limited by serious side effects. We have screened a small portion of a unique chemical library and have found at least three novel compounds that are effective against L. tarentolae and L. major in vitro and in a murine macrophage model of L. major infection. These compounds were effective in both assays at doses significantly lower than those of sodium stibogluconate (Pentostam) and represent possible candidates for drug development.
摘要
硕大利什曼原虫是一种重要的锥虫病原体，可引发利什曼病，该病在旧大陆的大部分地区都是一种严重疾病。目前的治疗方法包括少数几种锑化合物，这些化合物虽有一定疗效，但因严重的副作用而受到限制。我们筛选了一个独特化学文库的一小部分，发现至少有三种新型化合物在体外以及在硕大利什曼原虫感染的小鼠巨噬细胞模型中对热带利什曼原虫和硕大利什曼原虫有效。这些化合物在两种试验中均有效，且有效剂量显著低于葡萄糖酸锑钠（喷他脒），是药物开发的潜在候选物。
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