Scholarlink

<p>The key material, 2-chlorobenzo[<i>h</i>]quinoline-3-carbaldehyde condensed with various active-methylene reagents to produce some benzo[<i>h</i>]quinoline-based heterocycles like pyrazolone, imidazolone, thiazolidine, pyrimidinone, and indolinone candidates. The insecticidal activities of synthesized substrates were evaluated against cowpea aphid, <i>Aphis craccivora</i>, adults and common house mosquito, <i>Culex pipiens</i> larvae. The results of toxicological bioassays demonstrated that compounds <b>9</b> and <b>11</b>, containing 2-thioxoimidazolidine and 2-thioxothiazolidine core, exhibited high insecticidal activity against <i>A. craccivora</i> adults with LC<sub>50</sub>s of 3.54 and 3.87&#xa0;µg/mL, and against <i>C. pipiens</i> larvae with LC<sub>50</sub>s of 1.61 and 1.83&#xa0;µg/mL, respectively. Schiff base <b>7</b> and arylidene <b>5</b> (bearing pyrazolone scaffolds) achieved good potencies with low LC<sub>50</sub> values of 4.40 and 5.25&#xa0;µg/mL for <i>A. craccivora</i> adults, and 2.16 and 2.49&#xa0;µg/mL for <i>C. pipiens</i> larvae, respectively. On the other hand, the bulky pyrimidinetrione <b>16</b> and indolone <b>18</b> showed low toxicities. Overall, the tested substrates were more effective against <i>C. pipiens</i> larvae than <i>A. craccivora</i> adults. The current study highlighted the effect of the inserted function groups on 2-chlorobenzo[<i>h</i>]quinoline core on the compounds’ activity through the structure-activity relationship (SAR) study. This study presents promising results for the development of novel and effective insecticides to be integrated into pest control programs.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Exploring insecticidal activity and SAR study of newly synthesized Benzo[h]quinoline-based heterocycles against Aphis craccivora Koch. and Culex pipiens L. Larvae

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年4月24日

查看全文
  • Eman A. E. El-Helw,
  • Doaa R. Abdel-Haleem,
  • Ali Kh. Khalil,
  • Sayed K. Ramadan

摘要

The key material, 2-chlorobenzo[h]quinoline-3-carbaldehyde condensed with various active-methylene reagents to produce some benzo[h]quinoline-based heterocycles like pyrazolone, imidazolone, thiazolidine, pyrimidinone, and indolinone candidates. The insecticidal activities of synthesized substrates were evaluated against cowpea aphid, Aphis craccivora, adults and common house mosquito, Culex pipiens larvae. The results of toxicological bioassays demonstrated that compounds 9 and 11, containing 2-thioxoimidazolidine and 2-thioxothiazolidine core, exhibited high insecticidal activity against A. craccivora adults with LC50s of 3.54 and 3.87 µg/mL, and against C. pipiens larvae with LC50s of 1.61 and 1.83 µg/mL, respectively. Schiff base 7 and arylidene 5 (bearing pyrazolone scaffolds) achieved good potencies with low LC50 values of 4.40 and 5.25 µg/mL for A. craccivora adults, and 2.16 and 2.49 µg/mL for C. pipiens larvae, respectively. On the other hand, the bulky pyrimidinetrione 16 and indolone 18 showed low toxicities. Overall, the tested substrates were more effective against C. pipiens larvae than A. craccivora adults. The current study highlighted the effect of the inserted function groups on 2-chlorobenzo[h]quinoline core on the compounds’ activity through the structure-activity relationship (SAR) study. This study presents promising results for the development of novel and effective insecticides to be integrated into pest control programs.