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De Novo Synthesis for MedChem on Sugars

MedChem 对糖的从头合成

基本信息

批准号：
7914474
负责人：
GEORGE A O'DOHERTY
金额：
$ 0.33万
依托单位：
WEST VIRGINIA UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2009
资助国家：
美国
起止时间：
2009-08-15 至 2010-08-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7914474
关键词：
Address Affect Aminoglycoside Antibiotics Anti-Bacterial Agents Antibiotics Antineoplastic Agents Belief Binding Biological Biological Factors Carbohydrates Cardiac Glycosides Chemistry Communicable Diseases Complex Coupled Deoxy Sugars Development Digitoxigenin Digitoxin Disease Enzymes Goals Isomerism Laboratories Libraries Macrolides Malignant Neoplasms Methodology Methods Monosaccharides Multi-Drug Resistance Mutation National Research Service Awards Nature Oligosaccharides Outcomes Research Palladium Pharmaceutical Chemistry Pharmaceutical Preparations Pharmacologic Substance Play Positioning Attribute Reaction Research Research Design Role Scheme Solubility Structure Structure-Activity Relationship Therapeutic Agents Tissues Transmembrane Transport Universities West Virginia Work analog anticancer activity antimicrobial antitumor agent bacterial resistance base cancer therapy carbohydrate structure cost drug discovery drug resistant bacteria empowered functional group glycosylation glycosyltransferase human disease improved landomycin A new technology novel novel strategies novel therapeutics programs resistant strain sugar

项目摘要

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.

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。