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Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety.
Küçükbay, Hasan; Gönül, Zeynep; Küçükbay, F Zehra; Angeli, Andrea; Bartolucci, Gianluca; Supuran, Claudiu T.
Afiliação
  • Küçükbay H; Department of Chemistry, Faculty of Arts and Sciences, Inönü University, Malatya, Turkey.
  • Gönül Z; Department of Chemistry, Faculty of Arts and Sciences, Inönü University, Malatya, Turkey.
  • Küçükbay FZ; Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy, Inönü University, Malatya, Turkey.
  • Angeli A; Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche E Nutraceutiche e Laboratorio Di Chimica Bioinorganica, Università Degli Studi Di Firenze, Florence, Italy.
  • Bartolucci G; Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche E Nutraceutiche e Laboratorio Di Chimica Bioinorganica, Università Degli Studi Di Firenze, Florence, Italy.
  • Supuran CT; Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche E Nutraceutiche e Laboratorio Di Chimica Bioinorganica, Università Degli Studi Di Firenze, Florence, Italy.
J Enzyme Inhib Med Chem ; 35(1): 1021-1026, 2020 Dec.
Article em En | MEDLINE | ID: mdl-32297533
ABSTRACT
New dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. While all compounds showed moderate to good in vitro CA inhibitory properties against hCA IX and hCA XII with inhibition constants in the micromolar level (37.7-86.8 and 2.0-8.6 µM, respectively), they did not show inhibitory activity against hCA I and hCA II up to 100 µM concentration. The antioxidant capacity of the peptide-dihydroquinolinone conjugates was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. Most of the synthesised compounds showed low antioxidant activities compared to the control antioxidant compounds BHA and α-tocopherol.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Picratos / Compostos de Bifenilo / Inibidores da Anidrase Carbônica / Anidrases Carbônicas / Quinolonas / Dipeptídeos / Antioxidantes Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Picratos / Compostos de Bifenilo / Inibidores da Anidrase Carbônica / Anidrases Carbônicas / Quinolonas / Dipeptídeos / Antioxidantes Idioma: En Ano de publicação: 2020 Tipo de documento: Article