Synthesis and Biological Evaluation of Novel Thiazolidinedione Analogues as 15-Hydroxyprostaglandin Dehydrogenase Inhibitors
- 29 June 2011
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 54 (14), 5260-5264
- https://doi.org/10.1021/jm200390u
Abstract
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.Keywords
This publication has 16 references indexed in Scilit:
- High-Affinity Inhibitors of Human NAD+-Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity RelationshipsPLOS ONE, 2010
- Synthesis and SAR of thiazolidinedione derivatives as 15-PGDH inhibitorsBioorganic & Medicinal Chemistry, 2010
- Rescue of Impaired Fracture Healing in COX-2−/− Mice via Activation of Prostaglandin E2 Receptor Subtype 4The American Journal of Pathology, 2009
- Prostaglandins, NSAIDs, and Gastric Mucosal Protection: Why Doesn't the Stomach Digest Itself?Physiological Reviews, 2008
- Misoprostol to treat postpartum haemorrhage: a systematic reviewBJOG: An International Journal of Obstetrics and Gynaecology, 2005
- The Impact of Cyclooxygenase-2 Mediated Inflammation on Scarless Fetal Wound HealingThe American Journal of Pathology, 2004
- New topical agents for hair growthClinics in Dermatology, 1988
- Studies on antidiabetic agents. II. Synthesis of 5-(4-(1-methylcyclohexylmethoxy)-benzyl)thiazolidine-2,4-dione (ADD-3878) and its derivatives.CHEMICAL & PHARMACEUTICAL BULLETIN, 1982
- Treatment of vasospastic disease with prostaglandin E1.BMJ, 1980
- The Biological Activities of Three Metabolites of Prostaglandin E1Acta Physiologica Scandinavica, 1966