1,2,3-三唑取代的1,4-二氢-4-氧代-1,5-二氮杂萘-3-羧酸衍生物的设计、合成与HIV整合酶抑制活性评价

一价铜催化端炔与叠氮化物的1, 3-环加成反应是一种快速构建小分子库并筛选其可能性质的的主要方法。本文报道了1,2,3-三唑取代的1,4-二氢-4-氧代-1,5-二氮杂萘-3-羧酸衍生物的设计与合成。在该类化合物中，疏水性与亲水性片段通过Click反应有效地连接。所设计化合物8和12的结构通过光谱手段进行了表征；其可能的HIV整合酶抑制活性也进行了筛选。

Design,Synthesis and Anti‐HIV Integrase Evaluation of 1,2,3‐ Triazol‐4‐yl‐substituted 1,4‐Dihydro‐4‐oxo‐1,5‐napthyridine‐ 3‐carboxylic Acids

Copper(I)‐catalyzed terminal alkyne‐azide 1,3‐cycloaddition reaction has emerged as one of the main strategies for the rapid creation and screening of a small molecular library. The present work describes the design and synthesis of a series of 1,2,3‐triazol‐4‐yl‐substituted 1,4‐dihydro‐4‐oxo‐1,5‐napthyridine‐3‐carboxylic acids in which the hydrophobic and hydrophilic domains were efficiently incorporated by a click reaction. The structures of the desired products 8 and 12 were characterized by spectroscopic methods and their HIV integrase inhibitory activities were also screened.