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从小类药品到口服活性皮佩拉-2,5-基环类药物的进步

Vladislav Deigin¹, Natalia Linkova², Olga Volpina¹

¹The Laboratory of Synthetic Vaccines of Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya St., 16/10, Moscow 117997, Russia.

International journal of molecular sciences

|September 9, 2023

概括

开发口服可用的类药物是一项挑战. 使用分支皮佩拉-2,5-二的新平台创建了稳定的peptidomimetics与保存的生物活性,用于口服.

科学领域:

药用化学医学化学
药物运输药物运输药物运输
酸科学酸科学

背景情况:

口服类药物仍然是药物开发中的一个重大障碍.
现有的方法往往在稳定性和生物可用性方面扎.
基于的药物具有治疗潜力,但在配方方面面临着挑战.

研究的目的:

引入一种新的化学平台,用于制造口服可用的类模拟剂.
为了证明小,活性的转化为口服稳定的化合物.
探索开发用于口服的短类药物.

主要方法:

一个化学平台的设计,基于分支的皮佩拉-2,5-.
片或生物活性分子通过链接器对生物载体进行共价附着.
制备具有特定生物活性的类仿制药.

主要成果:

成功创建了一种口服可用的皮多米米特平台.
在口服的化合物中证明了生物活性的保存.
合成的模仿药物表现出血红刺激,血红抑制和辅助活性.
观察到对等分子中的互惠生物活性.

结论:

开发的平台可以通过口服提供基于的治疗方法.
这种方法有助于活性转化为口服稳定的药物.
这项研究突出了类药物开发的进化路径,指向口服环和类模拟剂.

关键词:

循环性型模仿学循环性型模仿学药物开发是药物的发展.免疫性类的免疫性类.相互活性的反反体.

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