中文摘要：

目的以艾滋病病毒（HW）gp41为作用靶点，设计合成了12个含芳基取代的苯甲酸类化合物，并对其进行抗HIV活性测试。方法以卤代苯甲酸或间羧基苯硼酸为原料，通过Suzuki-Miyaura偶连反应及Knoevenagel缩合反应，引入含取代基的芳环及芳杂环。ELISA法检测其抑制HIV gp41六螺旋束形成的活性。荧光素酶法检测化合物抗HIV活性。结果化合物结构经NMR、MS得到确认，其中5个化合物（7b、7c、7d、7e、7g）具有抑制HIVgp41六螺旋束形成的活性，其中7d活性最强。该化合物能抑制HIV-1SF33病毒株的复制，其IC50为20μmol／L。结论合成的芳基苯甲酸类化合物7d能通过抑制HIV gp41六螺旋束结构的形成来抑制HIv的复制。

英文摘要：

Objective To synthesize novel aryl-substituent benzyl acid compounds targeting HIV gp41 and characterize their anti-HIV activities. Methods Twelve analogues of aryl-substituent benzyl acid were designed and synthesized by Suzuki- Miyaura cross-coupling and Knoevenagel condensation reactions using halo-benzyl acid or 3-carboxybenzeneboronic acid as the raw material. The inhibitory activities of these compounds on gp41 six-helix bundle formation were tested by ELISA, and their anfi-HW activities were determined using a luciferase assay. Results The structures of the compounds were characterized by nuclear magnetic resonance and mass spectrography. Among the 12 compounds, 5 （7b, 7c, 7d, 7e, and 7g） could inhibit the gp41 six-helix bundle formation, and 7d showed the most potent effect, and could also inhibit the replication of HIV-1 SF33 strain with an ICs0 of 20 μmol/L. Conclusion The synthesized aryl-substituent benzyl acid compound 7d could inhibit HIV replication by blocking the gp41 six-helix bundle formation.