Development of anti-HIV agents targeting dynamic supramolecular mechanism and feedback mechanism

在治疗HIV传染病和艾滋病的药物开发中，我们合成了具有动态超分子机制的HIV进入抑制剂如CXCR4拮抗剂和其他具有不同作用机制的新型药物。1. 开发了具有二甲苯支架的新型CXCR4拮抗剂和有效的二价CXCR4拮抗剂。2. 小的CD4模拟衍生物对HIV进入具有显著的抑制活性，并引起对中和抗体的结合亲和力增加。3. 从Vpr片段中发现整合酶抑制剂。4. 从具有细胞膜穿透信号的基质片段中衍生出抗hiv药物。

In the development of drugs for treatments of HIV infectious disease and AIDS, we have synthesized HIV entry inhibitors having dynamic supramolecular mechanism such CXCR4 antagonists and other novel agents having different action mechanism. 1. Novel CXCR4 antagonists having xylene scaffold and potent bivalent CXCR4 antagonists were developed. 2. Small CD4 mimic derivatives having significant inhibitory activity against HIV entry and causing an increase of binding affinity for neutralizing antibodies were found. 3. Integrase inhibitors were discovered from Vpr fragments. 4. Anti-HIV agents derived from matrix fragments with cell membrane penetrating signals were developed.