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Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes i and II
- Publication Year :
- 2012
- Publisher :
- Informa Healthcare, 2012.
-
Abstract
- Mannich bases 2a-f derived from 3,4-dimethylphenol (1), formaldehyde and different amines are prepared and subjected to spectral (IR, 1H and 13C NMR) and elemental analyses. The inhibition of two human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II, with 1 and synthesized Mannich bases 2a-f and acetazolamide (AAZ) as a control compound was investigated in vitro by using the hydratase and esterase assays. In relation to hydratase and esterase activities of the half maximal inhibitory concentration (IC50) and the inhibition equilibrium constants (Ki)values were determined. Only two compounds (2a and 2e)exhibit weak hCA II inhibitory effects on esterase activity. IC50 and Ki values for 2a and 2e with respect to esterase activity of hCA II are0.88 × 103 and 6.3-7.6 µM and 0.44 × 103 and 19.0-96.4 µM,respectively. On the contrary, compounds 2b and 2d might be used as CA activators due to increasing esterase activity of hCA I and hCA II isozymes. © 2013 Informa UK, Ltd.<br />This work was supported by grant (Grant No: 2008-1) from the Dumlupınar University Research Foundation and carried out in the Department of Chemistry of the Dumlupınar University.
- Subjects :
- Erythrocytes
Stereochemistry
Formaldehyde
Mannich base
Xylenes
Isozyme
Esterase
chemistry.chemical_compound
Structure-Activity Relationship
Carbonic anhydrase
Drug Discovery
medicine
Structure–activity relationship
Humans
Protein Isoforms
Amines
Carbonic Anhydrase Inhibitors
Carbonic Anhydrases
Pharmacology
biology
Dose-Response Relationship, Drug
Molecular Structure
3,4-dimethylphenol
General Medicine
Carbon-13 NMR
NMR
Hydratase and esterase activities
chemistry
biology.protein
Acetazolamide
medicine.drug
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....231724ab5fb761afc702489cf8ea4adc