Indole Analogs as Novel Appetite Suppressants

肥胖影响着美国和世界各地数百万人，这种疾病对我们的社会产生了巨大的健康和经济后果。现有的治疗方法显示出有限的疗效，可能具有令人不安的副作用，并且通常需要长期治疗。发现一种新的治疗肥胖症的方法将具有非常可观的科学和商业价值。食欲抑制的药物治疗方法之一是开发5-HT 2C受体激动剂，这是我们第一阶段工作的重点。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）程序来优化和进一步开发这些先导化合物。从这个项目中，我们的具体目标是发现一种或多种吲哚类似物在我们的动物模型中表现出与批准的药物相同或更好的食欲抑制功效。此类先导物还将显示有利的药物样性质。该项目的长期目标是发现一种新的、改进的用于治疗肥胖症的药剂，该药剂可以被许可并开发用于最终的市场批准。7.在美国，肥胖是一个严重的健康问题，现有的帮助人们减肥的药物往往效果不佳，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，医生们将有另一种选择来帮助肥胖的人解决他们的体重问题。

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.