Design and development of novel series of indole‐3‐sulfonamide ureido derivatives as selective carbonic anhydrase II inhibitors
Autor: | Claudiu T. Supuran, Abhishek Choli, Andrea Angeli, Priti Singh, Mohammed Arifuddin, Venkata Madhavi Yaddanapudi, Baijayantimala Swain, Santosh K. Sahoo |
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Rok vydání: | 2021 |
Předmět: |
Indoles
Stereochemistry Carbonic anhydrase II Pharmaceutical Science Chemical synthesis Structure-Activity Relationship Drug Development Carbonic anhydrase Drug Discovery medicine Humans Urea Moiety Carbonic Anhydrase Inhibitors Indole test chemistry.chemical_classification Sulfonamides biology Chemistry Sulfonamide Isoenzymes Drug Design biology.protein Urea derivatives Acetazolamide medicine.drug |
Zdroj: | Archiv der Pharmazie. 355:2100333 |
ISSN: | 1521-4184 0365-6233 |
Popis: | Indole is a privileged moiety with a wide range of bioactivities, making it a popular scaffold in drug design and development studies as well as in synthetic chemistry. Here, novel urea derivatives of indole, containing sulfonamide at position-3 of indole, were synthesized using a well-known tail approach, as carbonic anhydrases (CAs; EC 4.2.1.1) inhibitors. All the newly synthesized molecules were screened for their CA-inhibitory activity against four clinically relevant isoforms of human-origin carbonic anhydrase (hCA), that is, hCA I, hCA II, hCA IX, and hCA XII. These compounds were specifically active against hCA II, more than against hCA I, hCA IX, and hCA XII. Derivative 6l was found to be most active, with a Ki value of 7.7 µM against hCA II. |
Databáze: | OpenAIRE |
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