单加氧酶类似物：吡唑并吡啶、苯并吡喃并吡唑并吡啶和氧桥唑嘧啶衍生物的合成及其生物筛选。
Monastrol analogs: a synthesis of pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged azolopyrimidine derivatives and their biological screening.
机构信息
Department of Pharmaceutical Analysis and Nuclear Pharmacy, Comenius University, Odbojarov 10, SK-832 32 Bratislava, Slovak Republic.
出版信息
Bioorg Med Chem Lett. 2010 Jul 15;20(14):4073-6. doi: 10.1016/j.bmcl.2010.05.085. Epub 2010 May 26.
A synthesis of novel pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged pyrazolo-, tetrazolo-, benzimidazo-, and thiazolopyrimidines via Hantzsch- and Biginelli-like condensations has been developed. The ability of these compounds to inhibit Eg5 activity has been examined. The results indicate that synthetic manipulations in the monastrol thiourea moiety are inefficient.
通过 Hantzsch-和 Biginelli 型缩合反应，合成了新型吡唑并吡啶、苯并吡喃并吡唑并吡啶以及氧桥连的吡唑并、四唑并、苯并咪唑并和噻唑并嘧啶类化合物。对这些化合物抑制 Eg5 活性的能力进行了研究。结果表明，在手性诱导剂单司他汀硫脲部分的合成操作效率低下。
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