Synthesis and Biological Evaluation of Novel Bromophenol Derivatives as Carbonic Anhydrase Inhibitors
作者： Yusuf Akbaba , Halis Türker Balaydın , Abdullah Menzek , Süleyman Göksu , Ertan Şahin
关键词:
摘要: Here, we provide an alternative synthesis of the natural bromophenol 3,4-dibromo-5-(2,3-dibromo-4,5-dihydroxybenzyl)-6-(ethoxymethyl)benzene-1,2-diol (3) and first (4,5-dihydroxy-2-methylphenyl)(3,4-dihydroxyphenyl)methanone (18) its brominated derivatives 19-21. The compounds were characterized tested against two most studied members pH regulatory enzyme family, carbonic anhydrase (CA). inhibitory potencies novel bromophenols 2, 3 analyzed at human isoforms hCA I II as targets KI values calculated. measured in range 13.7-32.7 mM for isozyme 0.65-1.26 isozyme. structurally related compound 14 was also order to understand structure–activity relationship, clinically used sulfonamide acetazolamide (AZA)was comparison reasons. All exhibited competitive inhibition with 4-nitrophenylacetate substrate. showed strong activity I, being more effective compared AZA (KI: 36.2 mM), but rather less II.
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