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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2008-11-25
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pubmed:abstractText |
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 subtypes 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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BaeMyung AeMA,
pubmed-author:BotezC ICI,
pubmed-author:CheonHyae GyeongHG,
pubmed-author:JunMi AeMA,
pubmed-author:KangNam SookNS,
pubmed-author:KangSeung KyuSK,
pubmed-author:KimKi YoungKY,
pubmed-author:KimKwang RokKR,
pubmed-author:KimSun YoungSY,
pubmed-author:KimSung GyuSG,
pubmed-author:KimSung SooSS,
pubmed-author:LeeDuck HyungDH,
pubmed-author:LeeJie OhJO,
pubmed-author:ParkWoul SeongWS,
pubmed-author:RheeSang DalSD,
pubmed-author:ShinMi SikMS,
pubmed-author:SohnSang KwonSK
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6525-9
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pubmed:meshHeading |
pubmed-meshheading:18996694-Binding Sites,
pubmed-meshheading:18996694-Chemistry, Pharmaceutical,
pubmed-meshheading:18996694-Crystallography, X-Ray,
pubmed-meshheading:18996694-Cytochrome P-450 CYP3A,
pubmed-meshheading:18996694-Diabetes Mellitus,
pubmed-meshheading:18996694-Dipeptidyl-Peptidase IV Inhibitors,
pubmed-meshheading:18996694-Drug Design,
pubmed-meshheading:18996694-Humans,
pubmed-meshheading:18996694-Inhibitory Concentration 50,
pubmed-meshheading:18996694-Models, Chemical,
pubmed-meshheading:18996694-Molecular Structure,
pubmed-meshheading:18996694-Piperazines,
pubmed-meshheading:18996694-Pyrazines,
pubmed-meshheading:18996694-Structure-Activity Relationship,
pubmed-meshheading:18996694-Triazoles
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.
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pubmed:affiliation |
Drug Discovery Division, Korea Research Institute of Chemical Technology, Yuseong-Gu, Daejeon 305-600, Republic of Korea. jhahn@krict.re.kr
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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