3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation
| Autor: | Abhay, Priti Singh, Claudiu T. Supuran, Kamtam Aashritha, Andrea Angeli, Baijayantimala Swain, Narayana Nagesh, Mohammed Arifuddin |
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| Rok vydání: | 2020 |
| Předmět: |
Gene isoform
Stereochemistry Clinical Biochemistry Pharmaceutical Science 01 natural sciences Biochemistry Structure-Activity Relationship Carbonic anhydrase Drug Discovery medicine CARBONIC ANHYDRASE XIII Potency Humans Carbonic Anhydrase Inhibitors Molecular Biology Biological evaluation Carbonic Anhydrases Oxadiazoles Sulfonamides biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry 0104 chemical sciences Isoenzymes 010404 medicinal & biomolecular chemistry Design synthesis Drug Design biology.protein Molecular Medicine Acetazolamide medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 37 |
| ISSN: | 1464-3405 |
| Popis: | A new series of benzenesulphonamide linked-1,3,4-oxadiazole hybrids (6a–s) has been synthesized and tested for their carbonic anhydrase inhibition against human (h) carbonic anhydrase (CA) isoforms hCA I, II, IX, and XIII. Fluorescence properties of some of the synthesized molecules were studied. Most of the molecules exhibited significant inhibitory power, comparable or better than the standard drug acetazolamide (AAZ) on hCA XIII. Out of 19 tested molecules, compound 6e (75.8 nM) was 3 times more potent than AAZ (250.0 nM) against hCA I, whereas compound 6e (15.4 nM), 6g (16.2 nM), 6h (16.4 nM) and 6i (17.0 nM) were found to be more potent than AAZ (17.0 nM) against isoform hCA XIII. It is anticipated that these compounds could be taken as the potential leads for the development of selective hCA XIII isoform inhibitors with improved potency. |
| Databáze: | OpenAIRE |
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