发现一种新型的非那雄胺和依立雄胺的杂合体作为 5α-还原酶抑制剂。
Discovery of a novel hybrid from finasteride and epristeride as 5α-reductase inhibitor.
机构信息
College of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 210032, China.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):475-8. doi: 10.1016/j.bmcl.2010.10.112. Epub 2010 Oct 28.
Abstract
Finasteride and epristeride both inhibit 5α-reductase with high potency via competitive and non-competitive mechanism, respectively. A new hybrid of finasteride and epristeride was designed as a new 5α-reductase inhibitor based on combination principles in medicinal chemistry. Human 5β-reductase was chosen as a plausible surrogate of 5α-reductase type II and the results indicate that although the hybrid compound possesses the main bulk of epristeride, its inhibitory mechanism is same as of finasteride. The hybrid turned out to be a potent 5α-reductase inhibitor in low IC(50) ranges.
摘要
非那雄胺和依立雄胺分别通过竞争性和非竞争性机制强效抑制 5α-还原酶。根据组合化学的原理，将非那雄胺和依立雄胺设计为一种新型的 5α-还原酶抑制剂。选择人 5β-还原酶作为 5α-还原酶 II 型的合理替代物，结果表明，尽管该混合化合物具有依立雄胺的主要部分，但它的抑制机制与非那雄胺相同。该混合物在低 IC50 范围内成为一种有效的 5α-还原酶抑制剂。
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