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Discovery of Low Nanomolar and Subnanomolar Inhibitors of the Mycobacterial beta-Carbonic Anhydrases Rv1284 and Rv3273

dc.contributor.authorBalaban, Alexandru T.
dc.contributor.authorGuzel, Ozlen
dc.contributor.authorScozzafava, Andrea
dc.contributor.authorSupuran, Claudiu T.
dc.contributor.authorSalman, Aydin
dc.contributor.authorMaresca, Alfonso
dc.date.accessioned2021-03-05T19:05:16Z
dc.date.available2021-03-05T19:05:16Z
dc.date.issued2009
dc.identifier.citationGuzel O., Maresca A., Scozzafava A., Salman A., Balaban A. T. , Supuran C. T. , "Discovery of Low Nanomolar and Subnanomolar Inhibitors of the Mycobacterial beta-Carbonic Anhydrases Rv1284 and Rv3273", JOURNAL OF MEDICINAL CHEMISTRY, cilt.52, ss.4063-4067, 2009
dc.identifier.issn0022-2623
dc.identifier.otherav_cd921651-a2d9-4c00-a9cd-2b2984ee9914
dc.identifier.othervv_1032021
dc.identifier.urihttp://hdl.handle.net/20.500.12627/136022
dc.identifier.urihttps://doi.org/10.1021/jm9004016
dc.description.abstractA series of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides has been derivatized by reaction with 2,4,6-trimethylpyrylium perchlorate, leading to pyridinium derivatives. The new sulfonamides were evaluated as inhibitors of two beta-carbonic anhydrases (CAs, EC 4.2.1.1) from Mycobaterium tuberculosis, Rv1284 and Rv3273. The whole series showed excellent nanomolar inhibitory activity, with several subnanomolar inhibitors being detected. Rv1284 and Rv3273 have potential for developing antimycobacterial agents with an alternate mechanism of action.
dc.language.isoeng
dc.subjectTemel Eczacılık Bilimleri
dc.subjectYaşam Bilimleri
dc.subjectBiyokimya
dc.subjectTemel Bilimler
dc.subjectSağlık Bilimleri
dc.subjectEczacılık
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectFarmakoloji ve Toksikoloji
dc.subjectFARMAKOLOJİ VE ECZACILIK
dc.subjectTemel Bilimler (SCI)
dc.subjectKimya
dc.subjectKİMYA, TIP
dc.titleDiscovery of Low Nanomolar and Subnanomolar Inhibitors of the Mycobacterial beta-Carbonic Anhydrases Rv1284 and Rv3273
dc.typeMakale
dc.relation.journalJOURNAL OF MEDICINAL CHEMISTRY
dc.contributor.departmentUniversity of Florence , ,
dc.identifier.volume52
dc.identifier.issue13
dc.identifier.startpage4063
dc.identifier.endpage4067
dc.contributor.firstauthorID192736


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