title: [Design, synthesis and activity assessment of aryl-substituent benzyl acid targeting HIV gp41].
abstract: 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 anti-HIV 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 IC(50) of 20 µmol/L.
  
  
  CONCLUSIONS
  The synthesized aryl-substituent benzyl acid compound 7d could inhibit HIV replication by blocking the gp41 six-helix bundle formation.
authors: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China. 183336049@qq.com
authors: Haibo
authors: H
authors: Wang
authors: Zhipeng
authors: Z
authors: Chen
authors: Jiayin
authors: J
authors: Qiu
authors: Xiaoling
authors: X
authors: Yu
authors: Yang
authors: Y
authors: Xie
authors: Shuwen
authors: S
authors: Liu
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects; D006841:Hydrocarbons, Aromatic / Q000138:chemical synthesis / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D019380:Anti-HIV Agents; D001565:Benzoates; D006841:Hydrocarbons, Aromatic