Development of a New Class of Pharmacological Mediators for Myeloperoxidase Inhib

说明(申请人提供)：心血管疾病是指涉及心脏或血管的疾病，特别是与动脉粥样硬化相关的疾病(动脉疾病)。这种疾病是世界各地的头号杀手，特别是在美国。髓过氧化物酶(MPO)与多种心血管疾病有关，目前尚无单一药物可用于治疗。髓过氧化物酶(MPO)候选新药的开发可能有助于防止脆弱的动脉粥样硬化斑块的进展。基于天然化学结构，我们建议开发一类新的抑制髓过氧化物酶的药理介体。我们的初步研究利用体外模型评估了两种特异性的MPO抑制剂。所建议的抑制剂的显著特征是这些抑制剂是针对MPO的，以及它们的通用抗氧化剂特性。可行性研究的具体目标如下：

DESCRIPTION (provided by applicant): Cardiovascular disease refers to the class of diseases that involve the heart or blood vessels especially those related to atherosclerosis (arterial disease). This disease is the number one killer around the world, particularly in the United States. Myeloperoxidase (MPO) enzyme has been implicated in many cardiovascular diseases and to date there is no single drug available for treatment. The development of new drug candidates against myeloperoxidase (MPO) may prove to be useful in the prevention of the progression of vulnerable atherosclerotic plaque. We propose the development of a new class of pharmacological mediators for myeloperoxidase inhibition based on naturally available chemical structures. Our preliminary studies identified two specific MPO inhibitors by evaluating their efficacy using in vitro model. The salient features of the proposed inhibitors are that these inhibitors are specific toward MPO as well as their generic anti oxidant properties. The feasibility study has specific aims as listed below: