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Keywords:

  • Suillus granulatus;
  • Anti-HIV activity;
  • Flazin analogues;
  • Flazinamide

Abstract

Flazin isolated from the fruiting bodies of Suillus granulatus was found to possess weak anti-HIV activity (EC50=2.36 μM, TI=12.1). To establish a SAR study, 46 flazin analogues were synthesized, and their anti-HIV activities were evaluated in vitro. Among them, flazinamide (9a) showed the most potent activity with an EC50 value of 0.38 μM and a TI value of 312.0. The results suggested that appropriate substituents at positions 3, 1′, and 5′ of flazin might play a crucial role in determining their anti-HIV activities, and that flazinamide can be considered as a promising, readily available anti-HIV agent.