Indole Analogs as Novel Appetite Suppressants

作为新型食欲抑制剂的吲哚类似物

• 批准号: 6797277
• 负责人: HOWARD P SARD
• 金额: $ 25.73万
• 依托单位: ORGANIX, INC.
• 依托单位国家: 美国
• 财政年份: 2003
• 资助国家: 美国
• 起止时间: 2003-09-01 至 2006-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6797277
• 关键词: analog; anorexic agent; drug design /synthesis /production; drug screening /evaluation; indoles; laboratory mouse

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 very considerable scientific and commercial value. We have discovered an indole derivative possessing an encouraging pharmacological profile as a potential appetite suppressant. In Phase One, we propose to synthesize carefully selected analogs of this active lead compound. The pharmacology of these compounds will be evaluated both in vitro and in vivo. From this project we specifically aim to discover one or more indole analogs showing efficacy in an animal model for appetite suppression comparable to that of established therapies. Such a result will strongly support continuation in Phase Two. The long-term goal of this project is to discover new, improved treatments for obesity.

描述（由申请人提供）：肥胖会影响美国和世界范围内数以百万计的人，这种疾病对我们的社会产生了巨大的健康和经济后果。现有治疗方法显示有限的功效，可能具有令人不安的副作用，并且通常需要长期治疗。发现肥胖的新疗法将具有非常大的科学和商业价值。我们发现了一种具有令人鼓舞的药理学特征作为潜在食欲抑制剂的吲哚衍生物。在第一阶段，我们建议合成该活性铅化合物的精心选择的类似物。这些化合物的药理学将在体外和体内进行评估。从这个项目中，我们特别旨在发现一个或多个吲哚类似物，显示动物模型中的疗效，以抑制与已建立疗法相当的食欲抑制。这样的结果将在第二阶段强烈支持延续。该项目的长期目标是发现新的，改进的肥胖治疗方法。