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Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
- Source :
- Molecules, Vol 26, Iss 7023, p 7023 (2021), Molecules, Volume 26, Issue 22
- Publication Year :
- 2021
- Publisher :
- MDPI AG, 2021.
-
Abstract
- A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) isoforms, hCA I and II (cytosolic enzymes) as well as hCA IX and XII (transmembrane, tumor-associated isoforms). Examples of isoform-selective inhibitors were obtained for all four enzymes investigated here, and a computational approach was employed for explaining the observed selectivity, which may be useful in drug design approaches for obtaining inhibitors with pharmacological applications useful as antiglaucoma, diuretic, antitumor or anti-cerebral ischemia drugs.
- Subjects :
- Gene isoform
medicine.medical_treatment
carbonic anhydrase
Pharmaceutical Science
Organic chemistry
Pyrazole
Article
Analytical Chemistry
chemistry.chemical_compound
QD241-441
Carbonic anhydrase
Neoplasms
Drug Discovery
inhibitors
medicine
Humans
pyrazole derivatives
Physical and Theoretical Chemistry
Carbonic Anhydrase Inhibitors
Carbonic Anhydrases
chemistry.chemical_classification
Sulfonamides
metalloenzymes
biology
Chemistry
Transmembrane protein
Neoplasm Proteins
Isoenzymes
Cytosol
Enzyme
Biochemistry
Chemistry (miscellaneous)
biology.protein
Molecular Medicine
Pyrazoles
Diuretic
Selectivity
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 26
- Issue :
- 7023
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....7576457fd385a98d9a4a0b7803b5eadf