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Inhibition survey with phenolic compounds against the δ- and η-class carbonic anhydrases from the marine diatom thalassiosira weissflogii and protozoan Plasmodium falciparum .
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 377-382. - Publication Year :
- 2020
-
Abstract
- The inhibition of δ- and η-class carbonic anhydrases (CAs; EC 4.2.1.1) was poorly investigated so far. Only one δ-CA, TweCA from the diatom Thalassiosira weissflogii, and one η-CA, PfCA, from Plasmodium falciparum , have been cloned and characterised to date. To enrich δ- and η-CAs inhibition profiles, a panel of 22 phenols was investigated for TweCA and PfCA inhibition. Some derivatives showed effective, sub-micromolar inhibition of TweCA (K <subscript>I</subscript> s 0.81-65.4 µM) and PfCA (K <subscript>I</subscript> s 0.62-78.7 µM). A subset of compounds demonstrated a significant selectivity for the target CAs over the human physiologically relevant ones. This study promotes the identification of new potent and selective inhibitors of TweCA and PfCA , which could be considered as leads for finding molecular probes in the study of carbon fixation processes (in which TweCA and orthologue enzymes are involved) or drug candidates in the treatment of malaria.
- Subjects :
- Antiprotozoal Agents chemical synthesis
Antiprotozoal Agents chemistry
Carbonic Anhydrase Inhibitors chemical synthesis
Carbonic Anhydrase Inhibitors chemistry
Dose-Response Relationship, Drug
Humans
Molecular Structure
Parasitic Sensitivity Tests
Phenols chemical synthesis
Phenols chemistry
Plasmodium falciparum enzymology
Structure-Activity Relationship
Antiprotozoal Agents pharmacology
Carbonic Anhydrase Inhibitors pharmacology
Carbonic Anhydrases metabolism
Diatoms enzymology
Phenols pharmacology
Plasmodium falciparum drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 35
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31856608
- Full Text :
- https://doi.org/10.1080/14756366.2019.1706089