Scholarlink

<p>Dehydroabietic acid (DHA) is a naturally occurring diterpene with relevant biological activities. 7-Oxodehydroabietic acid as a highly oxidized state derivative from Dehydroabietic acid (DHA) showing good activities. However, the reported compounds did not include triazole derivatives. To discover novel potent anti-inflammatory diterpenoids, a series of hybrids of 7-Oxodehydroabietic acid containing 1,2,3-triazole moiety were designed and synthesized. The anti-inflammatory activity of the new compounds was assessed towards BV2 cell lines using L-NMMA (IC<sub>50</sub> = 42.36 ± 2.47 <i>µ</i>M) as a positive control. Compared with the L-NMMA, anti-inflammatory effect (NO inhibitory activities) was found in these novel molecules, especially compounds <b>9</b> (IC<sub>50</sub> = 8.00 ± 0.83 <i>µ</i>M), <b>10</b> (IC<sub>50</sub> = 8.44 ± 0.89 <i>µ</i>M), <b>15</b> (IC<sub>50</sub> = 8.13 ± 0.97 <i>µ</i>M) and <b>16</b> (IC<sub>50</sub> = 8.84 ± 1.10 <i>µ</i>M). The anti-inflammatory activity of compounds <b>9</b>, <b>10</b>, <b>15</b> and <b>16</b> in vivo are underway.</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

Synthesis and anti-inflammatory activity of novel 1,2,3-triazole- derivatives from 7-Oxodehydroabietic acid

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年4月2日

查看全文
  • Yong-Feng Lv,
  • Fu-Cai Ren,
  • Kang Hui,
  • Jie Zheng,
  • Shou-Jin Liu,
  • Han Luo

摘要

Dehydroabietic acid (DHA) is a naturally occurring diterpene with relevant biological activities. 7-Oxodehydroabietic acid as a highly oxidized state derivative from Dehydroabietic acid (DHA) showing good activities. However, the reported compounds did not include triazole derivatives. To discover novel potent anti-inflammatory diterpenoids, a series of hybrids of 7-Oxodehydroabietic acid containing 1,2,3-triazole moiety were designed and synthesized. The anti-inflammatory activity of the new compounds was assessed towards BV2 cell lines using L-NMMA (IC50 = 42.36 ± 2.47 µM) as a positive control. Compared with the L-NMMA, anti-inflammatory effect (NO inhibitory activities) was found in these novel molecules, especially compounds 9 (IC50 = 8.00 ± 0.83 µM), 10 (IC50 = 8.44 ± 0.89 µM), 15 (IC50 = 8.13 ± 0.97 µM) and 16 (IC50 = 8.84 ± 1.10 µM). The anti-inflammatory activity of compounds 9, 10, 15 and 16 in vivo are underway.