De Novo Synthesis for MedChem on Sugars

本文提出了从头合成新化学的发展方向。 碳水化合物及其在合成新生物活性物质中的应用 分子。这些新的生物活性结构可能对一系列 疾病。这项建议的重点是抗癌和抗菌化合物。这个 治疗癌症的方法是使用这种新的方法来进行新的合成孔径雷达研究 已知的具有抗癌活性的天然产物中的碳水化合物部分。这 将对洋地黄毒素、SL0101和 关于抗菌药物，这项提议的重点是 解决细菌耐药性问题。 这项建议的主要目标是开发一种简明的方法 对于非天然糖，开发一种将非天然糖组装成 非天然低聚糖并将这些非天然糖结合到碳水化合物中 抗生素等。具有这些抗生素/抗肿瘤的非天然糖类似物 试剂将极大地帮助揭示哪些官能团对这些 分子相互作用，进而有助于制备更有效的新药物。

Proposed herein is the development of new chemistry for the de novo synthesis of carbohydrates and the use of this new methodology for the synthesis of new bioactive molecules. These new bioactive structures may have activities against a range of diseases. This proposal is focus on anticancer and antibacterial compounds. The approach toward cancer is to use this new methodology to preform novel SAR studies on the carbohydrate portion of known natural products with anticancer activity. This approach will be conducted on the carbohydrate portions of digitoxin, SL0101 and Landomycin A. With regard to antibacterial agents this proposal is focused on addressing the problem of bacterial resistance. The major objectives of this proposal are to develop a concise methodology toward unnatural sugars, to develop a method for the assembly of unnatural sugars into unnatural oligosaccharides and to incorporate these unnatural sugars into carbohydrate based antibiotics, etc. Having unnatural sugar analogues of these antibiotics/antitumor agents would greatly aid in revealing which functional groups are important to these molecular interactions and in turn help prepared new more potent drugs.