Literature DB >> 26928426

Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase.

Dilan Ozmen Ozgun1, Cem Yamali2, Halise Inci Gul2, Parham Taslimi3, Ilhami Gulcin3,4, Telat Yanik5, Claudiu T Supuran6.   

Abstract

The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1-P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1-P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2-5.9 times better inhibitors than clinically used drug Tacrine.

Entities:  

Keywords:  Acetylcholinesterase; Mannich bases; butyrylcholinesterase; carbonic anhydrase; isatin

Mesh：

Substances：

Year:  2016        PMID： 26928426     DOI： 10.3109/14756366.2016.1149479

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN： 1475-6366            Impact factor:   5.051


  13 in total

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2.  Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase.

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Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-21       Impact factor: 5.051

3.  Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors.

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4.  Molecular Modeling and In Vitro Studies of a Neutral Oxime as a Potential Reactivator for Acetylcholinesterase Inhibited by Paraoxon.

Authors:  Reuel L de Paula; Joyce S F D de Almeida; Samir F A Cavalcante; Arlan S Gonçalves; Alessandro B C Simas; Tanos C C Franca; Martin Valis; Kamil Kuca; Eugenie Nepovimova; José M Granjeiro
Journal:  Molecules       Date:  2018-11-12       Impact factor: 4.411

5.  Synthesis and bioactivity of several new hetaryl sulfonamides.

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Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

6.  Isatin: a privileged scaffold for the design of carbonic anhydrase inhibitors.

Authors:  Claudia Melis; Rita Meleddu; Andrea Angeli; Simona Distinto; Giulia Bianco; Clemente Capasso; Filippo Cottiglia; Rossella Angius; Claudiu T Supuran; Elias Maccioni
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-24       Impact factor: 5.051

7.  Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.

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8.  Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones.

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Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

9.  In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon.

Authors:  Daniel A S Kitagawa; Samir F de A Cavalcante; Reuel L de Paula; Rafael B Rodrigues; Leandro B Bernardo; Munique C J da Silva; Thiago N da Silva; Wellington V Dos Santos; José M Granjeiro; Joyce S F D de Almeida; Marcos C Barcellos; Ana Beatriz de A Correa; Tanos C C França; Kamil Kuča; Alessandro B C Simas
Journal:  Biomolecules       Date:  2019-10-08

10.  Synthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action.

Authors:  Mehmet Oguz; Erbay Kalay; Suleyman Akocak; Alessio Nocentini; Nebih Lolak; Mehmet Boga; Mustafa Yilmaz; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
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