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Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.
Soyer, Zeynep; Uysal, Sirin; Parlar, Sulunay; Tarikogullari Dogan, Ayse Hande; Alptuzun, Vildan.
Afiliação
  • Soyer Z; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ege University , Bornova , Izmir , Turkey.
  • Uysal S; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ege University , Bornova , Izmir , Turkey.
  • Parlar S; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ege University , Bornova , Izmir , Turkey.
  • Tarikogullari Dogan AH; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ege University , Bornova , Izmir , Turkey.
  • Alptuzun V; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ege University , Bornova , Izmir , Turkey.
J Enzyme Inhib Med Chem ; 32(1): 13-19, 2017 Dec.
Article em En | MEDLINE | ID: mdl-27766908
ABSTRACT
A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC50= 1.35 ± 0.08 µM), while compound 3 exhibited the highest inhibition against BuChE (IC50= 13.41 ± 0.62 µM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ftalimidas / Acetilcolinesterase / Sulfonamidas / Butirilcolinesterase / Inibidores da Colinesterase / Simulação de Acoplamento Molecular Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Turquia País de publicação: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ftalimidas / Acetilcolinesterase / Sulfonamidas / Butirilcolinesterase / Inibidores da Colinesterase / Simulação de Acoplamento Molecular Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Turquia País de publicação: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM