期刊
BIOORGANIC CHEMISTRY
卷 56, 期 -, 页码 75-82出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2014.07.009
关键词
Benzyl amine; Carbonic anhydrase; Enzyme inhibition; Sulfamide; Sulfamoyl carbamate; Molecular modeling
资金
- Scientific and Technological Research Council of Turkey (TUBITAK) [TBAG-109T241]
- Ataturk University
- Deanship of Scientific Research King Saud University [RGP-VPP-254]
- Science Academy, Turkey under the BAGEP program
In this study, a series of sulfamoyl carbamates and sulfamide derivatives were synthesized. Six commercially available benzyl amines and BnOH were reacted with chlorosulfonyl isocyanate (CSI) to give sulfamoyl carbamates. Pd-C catalyzed hydrogenolysis reactions of carbamates afforded sulfamides. The inhibition effects of novel benzylsulfamides on the carbonic anhydrase I, and II isoenzymes (CA I, and CA II) purified from fresh human blood red cells were determined by Sepharose-4B-L-Tyrosine-sulfanilamide affinity chromatography. In vitro studies were shown that all of novel synthesized benzylsulfamide analogs inhibited, concentration dependently, both hCA isoenzyme activities. The novel benzylsulfamide compounds investigated here exhibited nanomolar inhibition constants against the two isoenzymes. K-i values were in the range of 28.48 +/- 0.01-837.09 +/- 0.19 nM and 112.01 +/- 0.01-268.01 +/- 0.22 nM for hCAI and hCA II isoenzymes, respectively. Molecular modeling approaches were also applied for studied compounds. (C) 2014 Elsevier Inc. All rights reserved.
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