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J Biochem Mol Toxicol ; 32(8): e22173, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29975450

RESUMO

In this study, we aimed to determine the inhibition effects of novel synthesized sulfamates (2a-g), sulfonamides (3b-f), carbonyl sulfonamides (3h and i), and carbonyl sulfamates (4h and 4i), which were tested against two human cytosolic carbonic anhydrase I and II isozymes (hCA I and II) and acetylcholinesterase (AChE) enzyme. For inhibition properties of allylic sulfamates, the half maximal inhibitory concentration (IC50 ) and inhibition constant (Ki ) were calculated for each novel compounds. The allylic sulfamates showed that Ki values are in the range of 187.33-510.31 pM for hCA I, 104.22-290.09 pM against hCA II, and 12.73-103.63 pM against AChE. The results demonstrated that all newly synthesized compounds had shown effective inhibition against hCA I and II isoenzymes and AChE enzyme.


Assuntos
Acetilcolinesterase/efeitos dos fármacos , Álcool Benzílico/química , Anidrase Carbônica II/efeitos dos fármacos , Anidrase Carbônica I/efeitos dos fármacos , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Colinesterase/farmacologia , Propanóis/química , Aminação , Citosol/enzimologia , Humanos , Concentração Inibidora 50
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