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Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors

Y Wu, S Karna, CH Choi, M Tong, HH Tai…

文献索引:Wu, Ying; Karna, Sandeep; Choi, Cheol Hee; Tong, Min; Tai, Hsin-Hsiung; Na, Dong Hee; Jang, Chul Ho; Cho, Hoon Journal of Medicinal Chemistry, 2011 , vol. 54, # 14 p. 5260 - 5264

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被引用次数: 26

摘要

Novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitors were synthesized. Compounds 2, 3, and 4 exhibited IC50 of 25, 8, and 19 nM, respectively. They also significantly increased levels of PGE2 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 ...