Journal
ARCHIV DER PHARMAZIE
Volume 349, Issue 6, Pages 466-474Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201600047
Keywords
Carbonic anhydrase; Enzyme inhibition; Enzyme purification; Isoenzyme
Funding
- Departments of Chemistry at Ataturk University
- TUBA (Turkish Academy of Sciences)
- Research Chairs Program at King Saud University
- EU
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N-substituted maleimides were synthesized from maleic anhydride and primary amines. 1,4-Dibromodibenzo[e,h]bicyclo-[2,2,2]octane-2,3-dicarboximide derivatives (4a-f) were prepared by the [4+2] cycloaddition reaction of dibromoanthracenes with the N-substituted maleimide derivatives. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new derivatives were assayed against the human (h) isozymes hCA I, II, IX, and XII. All tested bicyclo dicarboximide derivatives exhibited excellent inhibitory effects in the nanomolar range, with K-i values in the range of 117.73-232.87 nM against hCA I and of 69.74-111.51 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and XII.
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