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Discovery of indole-3-acetic acid derivatives containing 1,3,4-thiadiazole thioether and amide moieties as novel antibacterial agents

  • Chenghao Tang,
  • Jiali Shao,
  • Chou Si,
  • Xiumei Yang,
  • Xiuhong Hu,
  • Pei Li,
  • Xiang Wang

摘要

A series of twenty one novel compounds derived from indole-3-acetic acid, the structure of which includes 1,3,4-thiadiazole, thioether, and amide moieties were designed, synthesized, and evaluated for their in vitro antibacterial activity against three bacterial strains. The bioassay results showed that among the synthesized compounds, N-{5-[(2-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl}-3-(1H-indol-3-yl)-propanamide demonstrated the best inhibition rate against Pseudomonas syringae pv. actinidiae and N-{5-[(4-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl}-3-(1H-indol-3-yl)propanamide possessed the best inhibition rate against Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri, in all cases superior to that of bactericides thiodiazole copper and bismerthiazol.