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Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold.
Salerno, Silvia; Amendola, Giorgio; Angeli, Andrea; Baglini, Emma; Barresi, Elisabetta; Marini, Anna Maria; Ravichandran, Rahul; Viviano, Monica; Castellano, Sabrina; Novellino, Ettore; Da Settimo, Federico; Supuran, Claudiu T; Cosconati, Sandro; Taliani, Sabrina.
Afiliación
  • Salerno S; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Amendola G; DiSTABiF, University of Campania Luigi Vanvitelli, Caserta, Italy.
  • Angeli A; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Florence), Italy.
  • Baglini E; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Barresi E; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Marini AM; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Ravichandran R; DiSTABiF, University of Campania Luigi Vanvitelli, Caserta, Italy.
  • Viviano M; Department of Pharmacy, Epigenetic Med Chem Lab, University of Salerno, Fisciano (SA), Italy.
  • Castellano S; Department of Pharmacy, Epigenetic Med Chem Lab, University of Salerno, Fisciano (SA), Italy.
  • Novellino E; Department of Pharmacy, University Federico II of Naples, Naples, Italy.
  • Da Settimo F; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Supuran CT; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Florence), Italy.
  • Cosconati S; DiSTABiF, University of Campania Luigi Vanvitelli, Caserta, Italy. Electronic address: sandro.cosconati@unicampania.it.
  • Taliani S; Department of Pharmacy, University of Pisa, Pisa, Italy.
Eur J Med Chem ; 220: 113490, 2021 Aug 05.
Article en En | MEDLINE | ID: mdl-33975138
Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the discovery of potential drugs devoid of off-target side effects. As a consequence, substantial efforts are still needed to allow for the full realization of the pharmacological potential of CA modulators. In this contribution, starting from our previous studies, we describe the synthesis of a set of new bicyclic tetrahydroindazoles featuring a secondary sulfonamide. Biological evaluation of the inhibitory activity against the hCA I, II, IV, and IX isoforms allowed drawing a structure-activity relationship profile that was rationalized through theoretical studies. This allowed dissecting the new molecules into the single portions influencing the zinc chelation properties and the selectivity profile thereby offering a new platform for the discovery of new isotype selective CA inhibitors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Compuestos Bicíclicos Heterocíclicos con Puentes / Indazoles Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2021 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Francia
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Compuestos Bicíclicos Heterocíclicos con Puentes / Indazoles Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2021 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Francia