新型噻唑烷二酮类似物的合成及作为 15-羟基前列腺素脱氢酶抑制剂的生物评价。
Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.
机构信息
Department of Polymer Science and Engineering, Chosun University, Gwangju 501-759, South Korea.
出版信息
J Med Chem. 2011 Jul 28;54(14):5260-4. doi: 10.1021/jm200390u. Epub 2011 Jun 29.
Novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitors were synthesized. Compounds 2, 3, and 4 exhibited IC(50) of 25, 8, and 19 nM, respectively. They also significantly increased levels of PGE(2) in A549 cells. To assess the influence of 15-PGDH inhibitor on cochlear blood flow (CBF), 2 was applied intravenously to guinea pigs. It increased their CBFs. Scratch wounds were also analyzed in confluent monolayers of HaCaT cells. Cells exposed to 4 showed significantly improved wound healing with respect to a control.
新型噻唑烷二酮类似物作为 15-羟基前列腺素脱氢酶（15-PGDH）抑制剂被合成。化合物 2、3 和 4 的 IC50 分别为 25、8 和 19 nM。它们还显著增加了 A549 细胞中 PGE2 的水平。为了评估 15-PGDH 抑制剂对耳蜗血流（CBF）的影响，2 被静脉内应用于豚鼠。它增加了它们的 CBF。划痕伤口也在 HaCaT 细胞的汇合单层中进行了分析。与对照相比，暴露于 4 的细胞显示出明显改善的伤口愈合。
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