DC Field | Value | Language |
---|---|---|
dc.contributor.author | Ahn, Jin Hee | ko |
dc.contributor.author | Park, Woul Seong | ko |
dc.contributor.author | Jun, Mi Ae | ko |
dc.contributor.author | Shin, Mi Sik | ko |
dc.contributor.author | Kang, Seung Kyu | ko |
dc.contributor.author | Kim, Ki Young | ko |
dc.contributor.author | Dal Rhee, Sang | ko |
dc.contributor.author | Bae, Myung Ae | ko |
dc.contributor.author | Kim, Kwang Rok | ko |
dc.contributor.author | Kim, Sung Gyu | ko |
dc.contributor.author | Kim, Sun Young | ko |
dc.contributor.author | Sohn, Sang Kwon | ko |
dc.contributor.author | Kang, Nam Sook | ko |
dc.contributor.author | Lee, Jie-Oh | ko |
dc.contributor.author | Lee, Duck Hyung | ko |
dc.contributor.author | Cheon, Hyae Gyeong | ko |
dc.contributor.author | Kim, Sung Soo | ko |
dc.date.accessioned | 2009-09-11T06:12:52Z | - |
dc.date.available | 2009-09-11T06:12:52Z | - |
dc.date.created | 2012-02-06 | - |
dc.date.created | 2012-02-06 | - |
dc.date.issued | 2008-12 | - |
dc.identifier.citation | BIOORGANIC MEDICINAL CHEMISTRY LETTERS, v.18, no.24, pp.6525 - 6529 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/10203/11150 | - |
dc.description.abstract | Compounds with homopiperazine skeleton are designed to find a potent DPP-IV inhibitor without inhibiting CYP. Thus a series of beta-aminoacyl-containing homopiperazine derivatives was synthesized and evaluated. Compounds with acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. More specifically, compound 7m showed nanomolar activity with no inhibition towards five sub-types of CYPs, was considered as a prototype for further derivatization. Based on its X-ray co-crystal structure with human DPP-IV, we identified compounds 7s and 7t which showed good in vitro activity, no CYP inhibition, and good selectivity. (C) 2008 Elsevier Ltd. All rights reserved. | - |
dc.description.sponsorship | This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program, Ministry of Education, Science and Technology, Korea. We thank the staff of the 4A and 6B beam lines of Pohang Accelerator Laboratory. | en |
dc.language | English | - |
dc.language.iso | en_US | en |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | GLUCAGON-LIKE PEPTIDE-1 | - |
dc.subject | GLUCOSE-TOLERANCE | - |
dc.subject | DISCOVERY | - |
dc.subject | DESIGN | - |
dc.subject | POTENT | - |
dc.title | Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors | - |
dc.type | Article | - |
dc.identifier.wosid | 000261141100051 | - |
dc.identifier.scopusid | 2-s2.0-56249143071 | - |
dc.type.rims | ART | - |
dc.citation.volume | 18 | - |
dc.citation.issue | 24 | - |
dc.citation.beginningpage | 6525 | - |
dc.citation.endingpage | 6529 | - |
dc.citation.publicationname | BIOORGANIC MEDICINAL CHEMISTRY LETTERS | - |
dc.identifier.doi | 10.1016/j.bmcl.2008.10.076 | - |
dc.embargo.liftdate | 9999-12-31 | - |
dc.embargo.terms | 9999-12-31 | - |
dc.contributor.localauthor | Lee, Jie-Oh | - |
dc.contributor.nonIdAuthor | Ahn, Jin Hee | - |
dc.contributor.nonIdAuthor | Park, Woul Seong | - |
dc.contributor.nonIdAuthor | Jun, Mi Ae | - |
dc.contributor.nonIdAuthor | Shin, Mi Sik | - |
dc.contributor.nonIdAuthor | Kang, Seung Kyu | - |
dc.contributor.nonIdAuthor | Kim, Ki Young | - |
dc.contributor.nonIdAuthor | Dal Rhee, Sang | - |
dc.contributor.nonIdAuthor | Bae, Myung Ae | - |
dc.contributor.nonIdAuthor | Kim, Kwang Rok | - |
dc.contributor.nonIdAuthor | Kim, Sung Gyu | - |
dc.contributor.nonIdAuthor | Kim, Sun Young | - |
dc.contributor.nonIdAuthor | Sohn, Sang Kwon | - |
dc.contributor.nonIdAuthor | Kang, Nam Sook | - |
dc.contributor.nonIdAuthor | Lee, Duck Hyung | - |
dc.contributor.nonIdAuthor | Cheon, Hyae Gyeong | - |
dc.contributor.nonIdAuthor | Kim, Sung Soo | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | Dipeptidyl peptidase IV | - |
dc.subject.keywordAuthor | Diabetes | - |
dc.subject.keywordAuthor | Inhibitor | - |
dc.subject.keywordAuthor | Homopiperazine | - |
dc.subject.keywordPlus | GLUCAGON-LIKE PEPTIDE-1 | - |
dc.subject.keywordPlus | GLUCOSE-TOLERANCE | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | POTENT | - |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.