dc.contributor.author | Mastrolorenzo, Antonio | |
dc.contributor.author | Muehlschlegel, Fritz A. | |
dc.contributor.author | Supuran, Claudiu T. | |
dc.contributor.author | Guezel, Oezlen | |
dc.contributor.author | Maresca, Alfonso | |
dc.contributor.author | Hall, Rebecca A. | |
dc.contributor.author | Scozzafava, Andrea | |
dc.date.accessioned | 2021-03-04T19:13:39Z | |
dc.date.available | 2021-03-04T19:13:39Z | |
dc.date.issued | 2010 | |
dc.identifier.citation | Guezel O., Maresca A., Hall R. A. , Scozzafava A., Mastrolorenzo A., Muehlschlegel F. A. , Supuran C. T. , "Carbonic anhydrase inhibitors. The beta-carbonic anhydrases from the fungal pathogens Cryptococcus neoformans and Candida albicans are strongly inhibited by substituted-phenyl-1H-indole-5-sulfonamides", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.20, ss.2508-2511, 2010 | |
dc.identifier.issn | 0960-894X | |
dc.identifier.other | av_8eb25e00-4f1a-4c67-905d-cf73e71332a6 | |
dc.identifier.other | vv_1032021 | |
dc.identifier.uri | http://hdl.handle.net/20.500.12627/96412 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmcl.2010.02.103 | |
dc.description.abstract | A series of 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides and 1-({[5-(aminosulfonyl)-3- phenyl-1H-indol-2-yl]carbonyl}amino)-2,4,6 trimethylpyridinium perchlorates possessing various 2-, 3- or 4-substituted phenyl groups with methyl-, halogeno- and methoxy-functionalities, as well as the perfluorophenyl moiety, have been evaluated as inhibitors of the beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic fungi Cryptococcus neoformans (Can2) and Candida albicans (CaNce103). Both enzymes were potently inhibited by these sulfonamides, K(I)s in the range of 4.4-118 nM against Can2, and of 5.1-128 against CaNce103, respectively. Minor structural changes in the 3- substituted phenyl moiety contribute significantly to the inhibitory activity. Some of the investigated sulfonamides showed promising selectivity ratios for inhibiting Can2 over the host, human enzymes CA I and II. (C) 2010 Elsevier Ltd. All rights reserved. | |
dc.language.iso | eng | |
dc.subject | Temel Eczacılık Bilimleri | |
dc.subject | KİMYA, TIP | |
dc.subject | Kimya | |
dc.subject | Temel Bilimler (SCI) | |
dc.subject | KİMYA, ORGANİK | |
dc.subject | FARMAKOLOJİ VE ECZACILIK | |
dc.subject | Farmakoloji ve Toksikoloji | |
dc.subject | Yaşam Bilimleri (LIFE) | |
dc.subject | Sağlık Bilimleri | |
dc.subject | Eczacılık | |
dc.subject | Yaşam Bilimleri | |
dc.subject | Biyokimya | |
dc.subject | Biyoinorganik Kimya | |
dc.subject | Temel Bilimler | |
dc.title | Carbonic anhydrase inhibitors. The beta-carbonic anhydrases from the fungal pathogens Cryptococcus neoformans and Candida albicans are strongly inhibited by substituted-phenyl-1H-indole-5-sulfonamides | |
dc.type | Makale | |
dc.relation.journal | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | |
dc.contributor.department | University of Florence , , | |
dc.identifier.volume | 20 | |
dc.identifier.issue | 8 | |
dc.identifier.startpage | 2508 | |
dc.identifier.endpage | 2511 | |
dc.contributor.firstauthorID | 195715 | |