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作为和二烯生物固醇的螺旋[3.3]乙烯

Kateryna Prysiazhniuk¹, Oleksandr P Datsenko¹, Oleksandr Polishchuk¹

¹Enamine Ltd., Winston Churchill Str. 78, 02094, Kyiv, Ukraine.

Angewandte Chemie (International ed. in English)

|January 22, 2024

概括

聚[3.3],一种和的基生物,被用来制造抗癌和麻醉药物的新型类似物. 这些无专利的化合物在生物测试中显示出高强度,为治疗提供了新的可能性.

科学领域:

药用化学医学化学
有机化学有机化学
药物发现药物发现药物发现

背景情况:

螺旋[3.3] 赫普坦支架提供了一个独特的三维结构,具有非共平面出口向量.
这种支架被确定为基环的和生物,这是制药中常见的动机.
用和生物异构体取代芳香环可以改变物理化学性质和代谢稳定性.

研究的目的:

在药物设计中探索螺旋[3.3]核作为基生物异体的实用性.
通过结合spiro[3.3]heptane支架,合成现有药物的新型类似物.
为了评估这些新的和类型的生物活性和功效.

主要方法:

设计和合成含有spiro[3.3]heptane的类似物.
在已知的药物 (sonidegib,vorinostat,benzocaine) 中,将螺旋[3.3]赫核心纳入环的位置.
生物测试以评估合成化合物的功效.

主要成果:

通过使用spiro[3.3]heptane支架成功合成了无专利类型.
在相关的生物测定中证明了这些和类型的高功效.
在抗癌和麻醉药物结构中,spir[3.3]heptane核心有效地取代了基.

结论:

螺旋基[3.3]基核是药物开发中环的可行的和生物异.
新型的,无专利的sonidegib,vorinostat和可因的类似物显示出显著的生物效能.
这种支架代表了开发具有改进性质的新疗法剂的有希望的战略.

关键词:

生物异体是生物异体循环布他的使用方法药用化学医学化学螺旋体[3.3] 七次体七次体螺旋环是螺旋环中的一个.

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