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: 6235030
• 负责人: LEROY B. TOWNSEND
• 金额: $ 16.68万
• 依托单位: UNIVERSITY OF MICHIGAN AT ANN ARBOR
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-08-01 至 1998-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6235030
• 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.

该提案概述了几个特定领域的开发 专门治疗人巨细胞病毒感染的试剂。目标化合物将是 根据具有以下特征的结构活动关系推选 已经从当前和以前的研究中建立了我们的 实验室。提出了几个研究领域和具体目标 未来五年包括以下内容：综合一些 多取代苯并咪唑和咪唑及其对应的 基于结构活性的核苷及其类似物 从结构上相关的化合物衍生出来的关系。该合成器 提出了几个精选的5-溴杀菌素和硫代血管万古霉素类似物。 非相关多取代苯并咪唑氨基甲酸酯的合成 对上述多取代苯并咪唑，使用一种已发现的化合物 通过我们非常有限的筛选，涉及从 我们之前的综合调查，作为我们的重点。试管苗 来自Drach、Lopatin和Kern教授的实验室的评估将是 用来指导每个新的潜在领域的化学修饰 探员们。所有这些研究都应该为我们提供一些关于 将提高这些化合物的选择性的修改 抗人巨细胞病毒的化合物。