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<p>Dengue, chikungunya, and Zika are major viral diseases transmitted by <i>Aedes aegypti</i> Linn. (Diptera: Culicidae). Vector control measures include the use of larvicides in breeding sites, which in turn induce the emergence of target-resistant strains and non-target undesirable effects. An alternative to avoid drawbacks caused by the use of these products is to develop new selective compounds with less impact on non-target species. Thus, 12 3-keto-substituted indole analogs were synthesized aiming to study their selectivity toward <i>Ae. aegypti</i> in preference to <i>Artemia salina</i> Linn. (Anostraca: Artemiidae). 3-Acyl-indole derivatives were synthesized by Friedel–Crafts acylation using acid chlorides, nitromethane, and fuming tin chloride in dichloromethane under nitrogen atmosphere at 0&#xa0;°C and evaluated on 3rd-instar <i>Ae. aegypti</i> and <i>A. salina</i>. Linear aliphatic derivatives exhibited potency alternation by increasing the number of CH<sub>2</sub> in the C3 chain for both <i>Ae. aegypti</i> and <i>A. salina</i>. (3-Chlorophenyl)1-(1<i>H</i>-indol-3-yl)methanone exhibited the highest larvicidal activity (LC<sub>50</sub> 197.4&#xa0;µM) against <i>Ae. aegypti</i> and demonstrated to be the most selective molecule, exhibiting suitability index (SI) &lt; 19.7.</p>

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Different susceptibilities of Aedes aegypti (Diptera: Culicidae) and Artemia salina (Anostraca: Artemiidae) to keto-indole derivatives: structural features enhancing selectivity

  • 期刊论文

  • 发表日期：

    2026年2月1日

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  • Thaysnara Batista Brito,
  • Rafael dos Reis Barreto de Oliveira,
  • Maria de Lourdes da Graça Macoris,
  • Roseli La Corte,
  • Sócrates Cabral de Holanda Cavalcanti

摘要

Dengue, chikungunya, and Zika are major viral diseases transmitted by Aedes aegypti Linn. (Diptera: Culicidae). Vector control measures include the use of larvicides in breeding sites, which in turn induce the emergence of target-resistant strains and non-target undesirable effects. An alternative to avoid drawbacks caused by the use of these products is to develop new selective compounds with less impact on non-target species. Thus, 12 3-keto-substituted indole analogs were synthesized aiming to study their selectivity toward Ae. aegypti in preference to Artemia salina Linn. (Anostraca: Artemiidae). 3-Acyl-indole derivatives were synthesized by Friedel–Crafts acylation using acid chlorides, nitromethane, and fuming tin chloride in dichloromethane under nitrogen atmosphere at 0 °C and evaluated on 3rd-instar Ae. aegypti and A. salina. Linear aliphatic derivatives exhibited potency alternation by increasing the number of CH2 in the C3 chain for both Ae. aegypti and A. salina. (3-Chlorophenyl)1-(1H-indol-3-yl)methanone exhibited the highest larvicidal activity (LC50 197.4 µM) against Ae. aegypti and demonstrated to be the most selective molecule, exhibiting suitability index (SI) < 19.7.