English to Chinese: Molecular Aspects of Medicinal Chemistry and Drug Design General field: Science Detailed field: Chemistry; Chem Sci/Eng | |
Source text - English Over the years, we've had an active program in the total and
semi-synthesis of antibiotics as well as in their chemical modification based on biological rationales.
Quantamycin, a computer-simulated inhibitor of ribosomal binding is an example of a successful, biologically inspired synthetic program (See topic 7).
Avermectin, a potent anthelmintic agent has been the target of total synthesis and chemical modification.
Other total syntheses of clinically important molecules include thienamycin, dihydromevinolin, ajmalicine, tetrahydrolipstatin, reserpine, among others.
A number of current research programs deal with the validation of biochemical hypotheses (mode of action, etc.) through rational design of models and novel drugs.
An active area of research involves the design of peptidomimetics, enzyme inhibitors, antagonists, novel β-lactams and β-lactamase inhibitors relying on structure-based design and available X-ray data.
Another area of current interest is the design and synthesis of RNA-binding molecules, including aminoglycoside antibiotics. | Translation - Chinese 在过去的数年中,我们已经建立了一套有效的体系,用于进行全合成或半合成抗生素,同时基于生物学原理的对其化学结构进行改造。
广达霉素,一个通过计算机模拟而发现的核糖体结合抑制剂,就是一个例子,一个成功的,受生物学启发的合成体系。
阿维菌素,一个强力驱虫剂,已经成为我们接下来的全合成和化学修饰的目标。
在其他同类药物中具有重大临床意义的分子全合成包括:噻烯霉素,二氢美唯喏霉素,阿吗碱,三氢制胰脂菌素,利血平
同时,很多目前的研究项目都在处理通过合理的模型和新药设计,以证实生物化学设想的有效性(如作用方式,等)
此外,一个活跃的研究领域,包括了关于多肽模拟物,酶抑制剂,拮抗剂,新的β-内酰胺和β-内酰胺酶抑制剂的药物设计,而这些药物的设计有赖于基于结构的设计和已有的X-ray数据
目前其他的研究兴趣是设计并合成与RNA结合的分子,包括氨基甙类抗菌素。 |