Literature DB >> 18406135

Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates.

Lei Fang1, Birgit Kraus, Jochen Lehmann, Joerg Heilmann, Yihua Zhang, Michael Decker.   

Abstract

Five tacrine-ferulic acid hybrids (6a-e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compounds have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, 6d showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the peripheral anionic site, whereas a reversible but competitive inhibitory action for butyrylcholinesterase. The antioxidant study revealed that four target compounds have, compared to Trolox, high ability to absorb reactive oxygen species.

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Year:  2008        PMID： 18406135     DOI： 10.1016/j.bmcl.2008.03.073

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  30 in total

Review 1.  Natural products as a source of Alzheimer's drug leads.

Authors:  Philip Williams; Analia Sorribas; Melanie-Jayne R Howes
Journal:  Nat Prod Rep       Date:  2010-11-12       Impact factor: 13.423

2.  Pd-catalyzed amination as an alternative to nucleophilic aromatic substitution for the synthesis of N-alkyltacrines and analogues.

Authors:  Ming Ma; Jimit Mehta; Larry D Williams; Paul R Carlier
Journal:  Tetrahedron Lett       Date:  2011-02-23       Impact factor: 2.415

3.  Synthesis and functional survey of new Tacrine analogs modified with nitroxides or their precursors.

Authors:  Tamás Kálai; Robin Altman; Izumi Maezawa; Mária Balog; Christophe Morisseau; Jitka Petrlova; Bruce D Hammock; Lee-Way Jin; James R Trudell; John C Voss; Kálmán Hideg
Journal:  Eur J Med Chem       Date:  2014-03-12       Impact factor: 6.514

4.  Elaborate ligand-based modeling coupled with QSAR analysis and in silico screening reveal new potent acetylcholinesterase inhibitors.

Authors:  Sawsan Abuhamdah; Maha Habash; Mutasem O Taha
Journal:  J Comput Aided Mol Des       Date:  2013-12-12       Impact factor: 3.686

5.  Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.

Authors:  Fouad H Darras; Beata Kling; Jörg Heilmann; Michael Decker
Journal:  ACS Med Chem Lett       Date:  2012-08-22       Impact factor: 4.345

6.  Predicting targets of compounds against neurological diseases using cheminformatic methodology.

Authors:  Katarina Nikolic; Lazaros Mavridis; Oscar M Bautista-Aguilera; José Marco-Contelles; Holger Stark; Maria do Carmo Carreiras; Ilaria Rossi; Paola Massarelli; Danica Agbaba; Rona R Ramsay; John B O Mitchell
Journal:  J Comput Aided Mol Des       Date:  2014-11-26       Impact factor: 3.686

7.  Modeling in vitro inhibition of butyrylcholinesterase using molecular docking, multi-linear regression and artificial neural network approaches.

Authors:  Fang Zheng; Max Zhan; Xiaoqin Huang; Mohamed Diwan M Abdul Hameed; Chang-Guo Zhan
Journal:  Bioorg Med Chem       Date:  2013-11-08       Impact factor: 3.641

Review 8.  Hybrids: a new paradigm to treat Alzheimer's disease.

Authors:  Manjinder Singh; Maninder Kaur; Navriti Chadha; Om Silakari
Journal:  Mol Divers       Date:  2015-09-02       Impact factor: 2.943

9.  Synthesis, pharmacological assessment, and molecular modeling of acetylcholinesterase/butyrylcholinesterase inhibitors: effect against amyloid-β-induced neurotoxicity.

Authors:  Daniel Silva; Mourad Chioua; Abdelouahid Samadi; Paula Agostinho; Pedro Garção; Rocío Lajarín-Cuesta; Cristobal de Los Ríos; Isabel Iriepa; Ignacio Moraleda; Laura Gonzalez-Lafuente; Eduarda Mendes; Concepción Pérez; María Isabel Rodríguez-Franco; José Marco-Contelles; M Carmo Carreiras
Journal:  ACS Chem Neurosci       Date:  2013-02-04       Impact factor: 4.418

10.  Acetylcholinesterase inhibitors with photoswitchable inhibition of β-amyloid aggregation.

Authors:  Xinyu Chen; Sarah Wehle; Natascha Kuzmanovic; Benjamin Merget; Ulrike Holzgrabe; Burkhard König; Christoph A Sotriffer; Michael Decker
Journal:  ACS Chem Neurosci       Date:  2014-03-14       Impact factor: 4.418
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