8cdx
From Proteopedia
Human carbonic anhydrase I complexed with 4-(3-ethylureido)benzenesulfonamide
Structural highlights
FunctionCAH1_HUMAN Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea.[1] Publication Abstract from PubMedSulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby, biphenyl- and benzylphenyl-substituted sulfonamides showed high selectivity against hCA IX and hCA XII; these enzymes are common targets in the treatment of hypoxic cancers, and noteworthy inhibitory activity was observed for several compounds toward hCA I that might be of interest for future applications to treat cerebral edema. Compound 3 (4-[3-(2-benzylphenyl)ureido]benzenesulfonamide) held an exceptionally low K(i) value of 1.0 nM for hCA XII. Ureidobenzenesulfonamides as Selective Carbonic Anhydrase I, IX, and XII Inhibitors.,Denner TC, Angeli A, Ferraroni M, Supuran CT, Csuk R Molecules. 2023 Nov 26;28(23):7782. doi: 10.3390/molecules28237782. PMID:38067512[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
| ||||||||||||||||||
