Journal
BIOORGANIC CHEMISTRY
Volume 77, Issue -, Pages 245-251Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.01.022
Keywords
Cyanoguanidines; Carbonic anhydrase; Isoforms; Isoform-selective inhibitor; Antiglaucoma agent
Funding
- ADYU BAP (Adiyaman University Scientific Research Projects Coordination Department) [ECZFMAP/2015-0002]
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A series of novel N,N ''-diaryl cyanoguanidines were synthesized by reacting diphenyl N-cyanocarbonimidate with sulfanilamide followed by treatment of the obtained cyano-O-phenylisourea with substituted aromatic amines. The newly prepared N,N ''-diaryl cyanoguanidines showed a very interesting inhibition profile against four selected human carbonic anhydrase (CA, EC 4.2.1.1) isoforms, hCA I and hCA II (cytosolic), hCA IV (membrane-bound), and hCA IX (transmembrane). All these compounds showed a potent inhibition against isoform hCA II,with inhibition constants in the low nanomolar range, as well as a high selectivity for hCA II over hCA I, IV and IX. Since hCA II is an important drug target for antiglaucoma agents, these isoform-selective inhibitors may be considered of interest for further medicinal/pharmacologic studies. (C) 2018 Elsevier Inc. All rights reserved.
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