| http://purl.uniprot.org/citations/32364386 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/32364386 | http://www.w3.org/2000/01/rdf-schema#comment | "Human carbonic anhydrase (CA; EC 4.2.1.1) isoforms II and VII are implicated in neuronal excitation, seizures, and neuropathic pain (NP). Their selective inhibition over off-target CAs is expected to produce an anti-NP action devoid of side effects due to promiscuous CA modulation. Here, a drug design strategy based on the observation of (dis)similarities between the target CA active sites was planned with benzenesulfonamide derivatives and, for the first time, a phosphorus-based linker. Potent and selective CA II/VII inhibitors were identified among the synthesized phenyl(thio)phosphon(amid)ates 3-22. X-ray crystallography depicted the binding mode of phosphonic acid 3 to both CAs II and VII. The most promising derivatives, after evaluation of their stability in acidic media, were tested in a mouse model of oxaliplatin-induced neuropathy. The most potent compound racemic mixture was subjected to HPLC enantioseparation, and the identification of the eutomer, the (S)-enantiomer, allowed to halve the dose totally relieving allodynia in mice."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.9b02135"xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Esposito D."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Alterio V."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "De Simone G."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Monti S.M."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Supuran C.T."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Ghelardini C."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Micheli L."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Di Cesare Mannelli L."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Buonanno M."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Gratteri P."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Bartolucci G."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Nocentini A."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Bua S."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Cirilli R."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Pierini M."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "ALOthman Z.A."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/author | "Osman S.M."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/date | "2020"xsd:gYear |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/pages | "5185-5200"xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/title | "Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy."xsd:string |
| http://purl.uniprot.org/citations/32364386 | http://purl.uniprot.org/core/volume | "63"xsd:string |