Indole Analogs as Novel Appetite Suppressants

描述（由申请人提供）：肥胖影响着美国和全世界数百万人，这种疾病对我们的社会造成了巨大的健康和经济后果。现有的治疗方法效果有限，可能会产生令人不安的副作用，而且往往需要长期治疗。发现一种治疗肥胖症的新方法将具有相当大的科学和商业价值。一种抑制食欲的药物治疗方法是开发5-HT2C受体激动剂，这是我们一期工作的重点。在第二阶段，我们建议通过合成和生物学评价的结构-活性关系（SAR）计划来优化和进一步开发这些先导物。从这个项目中，我们的目标是发现一种或多种吲哚类似物，在我们的动物模型中显示出与批准的药物相同或更好的食欲抑制效果。这样的铅也会显示出有利的药物性质。该项目的长期目标是发现一种新的、改进的治疗肥胖的药物制剂，并获得许可和开发，最终获得市场批准。7. 肥胖在美国是一个严重的健康问题，现有的帮助人们减肥的药物往往没有效果，而且有副作用。我们正在进行研究，以发现和开发一种治疗肥胖症的新药。如果我们成功了，医生将有另一种选择来帮助肥胖者解决体重问题。

DESCRIPTION (provided by applicant): Obesity affects millions of people in the U.S. and worldwide, and this disease has enormous health and economic consequences for our society. Existing treatments show limited efficacy, can possess troubling side effects, and often require long-term therapy. Discovery of a new treatment for obesity would have a very considerable scientific and commercial value. One approach to pharmacotherapy for appetite suppression is the development of 5-HT2C receptor agonists, which was the focus of our Phase One work. In Phase Two, we propose to optimize and further develop these leads through a Structure-Activity Relationship (SAR) program of synthesis and biological evaluation. From this project we specifically aim to discover one or more indole analogs showing efficacy in our animal model for appetite suppression that is equal to or better than approved medications. Such leads will also display favorable drug-like properties. The long-term goal of this project is to discover a new, improved pharmaceutical agent for treatment of obesity that can be licensed and developed for ultimate market approval. 7. Project Narrative Obesity is a serious health problem in the Unites States, and the existing drugs to help people lose weight are often not effective and have side effects. We are carrying out research to discover and develop a new drug for obesity. If we are successful, doctors will have another option to help obese people with their weight problem.