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Synthesis of two phloroglucinol derivatives with cinnamyl moieties as inhibitors of the carbonic anhydrase isozymes I and II: an in vitro studyBurmaoğlu, SerdarDilek, EsraYılmaz, Ali OsmanSupuran, Claudiu T.Enzyme inhibitionhuman CAIhuman CAIIphloroglucinolsynthesisCarbonic Anhydrase ICarbonic Anhydrase IICarbonic Anhydrase InhibitorsChromatography, AffinityCinnamatesDose-Response Relationship, DrugErythrocytesHumansIn Vitro TechniquesIsoenzymesMolecular StructureStructure-Activity Relationship4 para methoxycinnamyl phloroglucinol4,6 bis para methoxycinnamyl phloroglucinolacetazolamidecarbonate dehydratase Icarbonate dehydratase IIferulic acidgallic acidnatural productpara coumaric acidpara hydroxybenzoicpara methoxycinnamyl alcoholpara methoxycinnamyl bromidephenolTwo cinnamyl-substituted phloroglucinols, 4-p-methoxycinnamyl phloroglucinol (9) and 4,6-bis-p-methoxycinnamyl phloroglucinol (10) were synthesized. Two carbonic anhydrases, human carbonic anhydrase I and II (hCA I and II), were purified. Kinetic interactions between these isozymes with 9 and 10 were investigated. These new compounds exhibited inhibitory effects on the hCA I and II enzymes’ activity in vitro. The combination of the inhibitory effects of both phloroglucinol and p-coumaric acid groups in a single compound was explored. However, relative to the inhibitory effects of the two groups separately, compounds 9 and 10 demonstrated comparable inhibitory effects. More effective inhibitors of CAs could be created by testing these compounds on other CA isozymes. © 2016 Informa UK Limited, trading as Taylor & Francis Group.Taylor and Francis Ltd2016Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/14743https://doi.org/10.1080/14756366.2016.11816261475-6366enJournal of Enzyme Inhibition and Medicinal Chemistryinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/14743