一系列环戊基环取代基有变化的7-脱氮-5'-去甲阿瑞吡坦霉素衍生物的合成及抗锥虫活性
Synthesis and antitrypanosomal activities of a series of 7-deaza-5'-noraristeromycin derivatives with variations in the cyclopentyl ring substituents.
作者信息
Seley K L, Schneller S W, Rattendi D, Lane S, Bacchi C J
机构信息
Department of Chemistry, Auburn University, Alabama 36849-5312, USA.
出版信息
Antimicrob Agents Chemother. 1997 Aug;41(8):1658-61. doi: 10.1128/AAC.41.8.1658.
Abstract
Previous work in our laboratories has suggested that (+)-5'-nor-7-deazaaristeromycin (compound 1) may represent a prototype structure for a series of compounds with significant antitrypanosomal activities. To test this possibility, a series of derivatives of compound 1 with changes in the cyclopentyl substituents (compounds 3 to 10) have been studied. Although some growth activity was obtained with the L-like compound 5, related compounds 3 and 7 had little or no activity below 100 microM. D-like compounds 4 and 6 showed some activity at or below 100 microM, but the most interesting finding was that both the D- and L-like compounds having a methyl substituent on the 4' position were most active.
摘要
我们实验室之前的工作表明，（+）-5'-去甲-7-脱氮阿糖胞苷（化合物1）可能是一系列具有显著抗锥虫活性的化合物的原型结构。为了验证这一可能性，我们研究了一系列化合物1的衍生物，这些衍生物的环戊基取代基发生了变化（化合物3至10）。虽然L型化合物5表现出一定的生长活性，但相关化合物3和7在100 microM以下几乎没有活性。D型化合物4和6在100 microM及以下表现出一定活性，但最有趣的发现是，在4'位具有甲基取代基的D型和L型化合物活性最高。
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本文引用的文献
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