Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 배윤수 | * |
dc.contributor.author | 최선 | * |
dc.contributor.author | 주정희 | * |
dc.date.accessioned | 2016-09-08T03:09:38Z | - |
dc.date.available | 2016-09-08T03:09:38Z | - |
dc.date.issued | 2016 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.issn | 1464-3391 | * |
dc.identifier.other | OAK-19227 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/232165 | - |
dc.description.abstract | We report the synthesis of novel 3-substituted 5-benzylidene-1-methyl-2-thiohydantoins 3, and their biological evaluation using NADPH oxidase (NOX) 1 and 4. Based on structural and pharmacophore analyses of known inhibitors such as hydroxypyrazole 2, we envisioned interesting 2-thiohydantoin compounds, 3-substituted 5-benzylidene-1-methyl-2-thiohydantoins 3 that would be expected to well match the structural features in 2. Efficient synthesis of eighteen target compounds 3 were achieved through the synthetic pathway of 4 -> 11 -> 3, established after consideration of several plausible synthetic pathways. The inhibitory activities of compounds 3 against NOX 1 and 4 were measured, with some of the target compounds showing similar or higher activities compared with reference 2; in particular, compounds 3bz, 3cz, and 3ez were found to be promising inhibitors of both NOX 1 and 4 with modest isozyme selectivities, which highlights the significance of the 2-thiohydantoin substructure for inhibition of NOX 1 and 4. This marks the first time these compounds have been applied to the inhibition of NOX enzymes. (C) 2016 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | * |
dc.subject | Thiohydantoin | * |
dc.subject | Benzylidene | * |
dc.subject | Aluminum chloride | * |
dc.subject | NADPH oxidase (NOX) | * |
dc.title | Synthesis and biological evaluation of 3-substituted 5-benzylidene-1-methyl-2-thiohydantoins as potent NADPH oxidase (NOX) inhibitors | * |
dc.type | Article | * |
dc.relation.issue | 18 | * |
dc.relation.volume | 24 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 4144 | * |
dc.relation.lastpage | 4151 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.bmc.2016.06.056 | * |
dc.identifier.wosid | WOS:000382305500020 | * |
dc.identifier.scopusid | 2-s2.0-84982107509 | * |
dc.author.google | Bae, Yun Soo | * |
dc.author.google | Choi, Sun | * |
dc.author.google | Park, Jung Jae | * |
dc.author.google | Joo, Jung Hee | * |
dc.author.google | Cui, Minghua | * |
dc.author.google | Cho, Hyunsung | * |
dc.author.google | Lee, Won Jae | * |
dc.author.google | Lee, Sang Hyup | * |
dc.contributor.scopusid | 배윤수(15031067200) | * |
dc.contributor.scopusid | 최선(8659831000) | * |
dc.contributor.scopusid | 주정희(7103414031;16052907000) | * |
dc.date.modifydate | 20240415133331 | * |