title: Isatin: a privileged scaffold for the design of carbonic anhydrase inhibitors.
abstract: The isatin scaffold is the constitutive fragment of several natural and synthetic bioactive molecules. Albeit several benzene sulphonamide-based carbonic anhydrase inhibitors (CAIs) have been reported, only recently isatin benzene sulphonamides have been studied and proposed as CAIs. In this study we have designed, synthesised, and evaluated the biological activity of a series of differently substituted isatin-based benzene sulphonamides which have been designed for the inhibition of carbonic anhydrase isoforms. The activity of all the synthesised compounds was evaluated towards human carbonic anhydrase I, II, IX, and XII isozymes. Our results indicate that the nature and position of substituents on the isatin ring can modulate both activity and isozyme selectivity.
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Claudia
authors: C
authors: Melis
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Rita
authors: R
authors: Meleddu
authors: b Dipartimento NEUROFARBA, Sezione di Scienze Farmaceutiche , Università degli Studi di Firenze , Sesto Fiorentino , Florence , Italy.
authors: Andrea
authors: A
authors: Angeli
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Simona
authors: S
authors: Distinto
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Giulia
authors: G
authors: Bianco
authors: c Istituto di Bioscienze e Biorisorse, CNR , Napoli , Italy.
authors: Clemente
authors: C
authors: Capasso
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Filippo
authors: F
authors: Cottiglia
authors: d Laboratorio NMR e Tecnologie Bioanalitiche, Sardegna Ricerche , Pula , CA , Italy.
authors: Rossella
authors: R
authors: Angius
authors: b Dipartimento NEUROFARBA, Sezione di Scienze Farmaceutiche , Università degli Studi di Firenze , Sesto Fiorentino , Florence , Italy.
authors: Claudiu T
authors: CT
authors: Supuran
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Elias
authors: E
authors: Maccioni
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D007510:Isatin / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007510:Isatin
keywords: Antitumour agents; carbonic anhydrase inhibitors; isatin hybrid molecules