HETEROCYCLIC COMPOUNDS AS SELECTIVE INHIBITORS OF HUMAN CYTOMEGALOVIRUS

杂环化合物作为人类巨细胞病毒的选择性抑制剂

• 批准号: 6295676
• 负责人: LEROY B. TOWNSEND
• 金额: $ 17.23万
• 依托单位: UNIVERSITY OF MICHIGAN AT ANN ARBOR
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-08-01 至 2000-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6295676
• 关键词: antiviral agents; benzimidazoles; cytomegalovirus; drug design /synthesis /production; imidazole; nucleoside analog; nucleosides; pyrimidine nucleosides; tubercidin

This proposal outlines several specific areas for the development of an agent to specifically treat HCMV infections. The target compounds will be elected on the basis of the structure activity relationships which have already been established from current and previous studies in our laboratory. Several areas of research are proposed and the specific aims for the next five years include the following: the synthesis of some polysubstituted benzimidazoles and imidazoles and their corresponding nucleosides and nucleoside analogs based on structure activity relationships derived from structurally related compounds. The synthesize of a few select 5-bromotubercidin and thiosangivamycin analogs is proposed. Synthesis of selected polysubstituted benzimidazole carbamates, unrelated to the above polysubstituted benzimidazoles, using a compound discovered through our very limited screen involving compounds selected at random from our previous synthetic investigations, as our focal point. The in vitro evaluations from Professors Drach, Lopatin and Kern's laboratories will be used to direct the chemical modifications in each new area of potential agents. All of these studies should provide some insights into the modifications which will effect an increase in the selectivity of these compounds against HCMV.

该提案概述了发展的几个具体领域 专门治疗 HCMV 感染的药物。 目标化合物将是 根据结构活动关系选出 根据我们当前和以前的研究已经确定 实验室。 提出了几个研究领域和具体目标 未来五年的目标包括： 综合一些 多取代苯并咪唑和咪唑及其相应的 基于结构活性的核苷和核苷类似物 源自结构相关化合物的关系。 综合 提出了一些选择的 5-溴结核菌素和硫代血管霉素类似物。 选定的多取代苯并咪唑氨基甲酸酯的合成，不相关 使用发现的化合物对上述多取代苯并咪唑进行 通过我们非常有限的筛选，涉及随机选择的化合物 我们之前的综合研究，作为我们的焦点。 体外 Drach、Lopatin 和 Kern 教授实验室的评估将 用于指导每个新的潜在领域的化学修饰 代理。 所有这些研究都应该提供一些见解 会影响这些选择性增加的修饰 抗HCMV的化合物。