Design, Synthesis and Evaluation of 6-Oxo-1, 6-dihydropyrimidine- 2,5-dicarboxamide Derivatives as MMP 13 Inhibitors.pdf
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Design, Synthesis and Evaluation of 6-Oxo-1, 6-dihydropyrimidine- 2,5-dicarboxamide Derivatives as MMP 13 Inhibitors.pdf
Chem.Res.Chin.Univ.2013,29(1),67—70 doi:10.1007/s40242-012-213l-2
Design,SynthesisandEvaluationof6-Oxo一1,6-dihydropyrimidine-
2,5-dicarboxamideDerivativesasMM P13Inhibitors
LUHai.bin,WANGShi.han,LIQing.minandWANGYong.sheng,
,.CollegeofPharmacy,JilinUniversity,Changchun130021.尸R.China,
2.ChangchunUniversityofChineseMedicine,Changchun130021, R.China
Abstract Wedesignedandsynthsizedaseriesofnovel6-oxo-1,6-dihydropyrimidine一2,5-dicarboxamidederivatives
andevaluatedtheirinhibitioneffectsonMMP3,MMP12na dMMP 13.Thepharmacologicalresultsshow thatthey
havepotentandhighlyselectiveactivityofinhibitingMMP13.
Keywords Matrixmetal1oproteinase13(MMPl3);Matrixmetalloproteinase(MMP);Inhibition
1 lntrOductiOn inhibitorsofMⅣIP13.
The synthetic M ⅣlPs inhibitors with low moleculra
Matrix metalloproteinases(MMPs) are a family of weightsareusedinthetreatmentofthesediseases.Theseinhi-
Zn.dependentendOpeptidasesinvolvedinthedegradationna d
bitorsgenerallyincludeazincbindinggroup(ZBG),capableto
repairofthemajorcomponentsoftheextracellularmatrixof efficientlychelatethecatalyticzincion.boundtoasubstrate-
connective tissuest1,2J
. These enzymesare involved in many
likefragmentdesignedtofittheS1primaryspecificitysubsite
physiologicalprocesses such as ovulation,embryogenesis, nadadjacentsubsitesL“J.Hydroxamateisconsideredtobethe
angiogenesis.cellulra differentiation,nadwound healingt3,4J.
mostef
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