Literature DB >> 18232655

Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.

Lei Fang, Dorothea Appenroth, Michael Decker, Michael Kiehntopf, Carolin Roegler, Thomas Deufel, Christian Fleck, Sixun Peng, Yihua Zhang, Jochen Lehmann.   

Abstract

In search of safer anti-Alzheimer drugs, 14 NO-donor-tacrine hybrids (1- 14) were synthesized and evaluated for their ability to inhibit cholinesterases and for vasorelaxation effects. Compounds 1- 13 showed good cholinesterases inhibitory activities in vitro, while 14, particularly, was highly selective, preferring butyrylcholinesterase rather than acetylcholinesterase. Four selected compounds (1, 9, 11, and 14) moderately relaxed the porcine pulmonary arteries in organ bath. In the hepatotoxicity study, significant hepatotoxicity was caused by tacrine but not by 9.

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Year:  2008        PMID： 18232655     DOI： 10.1021/jm701491k

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

1.  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

2.  Design, Synthesis and Evaluation of Bifunctional Acridinine-Naphthalenediimide Redox-Active Conjugates as Antimalarials.

Authors:  Srikanta Dana; Sudhir Kumar Keshri; Jyoti Shukla; Kunwar Somesh Vikramdeo; Neelima Mondal; Pritam Mukhopadhyay; Suman Kumar Dhar
Journal:  ACS Omega       Date:  2016-09-01

Review 3.  Propargylamine-derived multitarget-directed ligands: fighting Alzheimer's disease with monoamine oxidase inhibitors.

Authors:  Irene Bolea; Alejandro Gella; Mercedes Unzeta
Journal:  J Neural Transm (Vienna)       Date:  2012-12-13       Impact factor: 3.575

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.  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

6.  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 7.  Organic Nitrate Therapy, Nitrate Tolerance, and Nitrate-Induced Endothelial Dysfunction: Emphasis on Redox Biology and Oxidative Stress.

Authors:  Andreas Daiber; Thomas Münzel
Journal:  Antioxid Redox Signal       Date:  2015-09-24       Impact factor: 8.401

8.  Synthesis and molecular modeling studies of cholinesterase inhibitor dispiro[indoline-3,2'-pyrrolidine-3',3''-pyrrolidines].

Authors:  M Adel Youssef; Siva S Panda; Riham A El-Shiekh; ElSayed M Shalaby; Dalia R Aboshouk; Walid Fayad; Nehmedo G Fawzy; Adel S Girgis
Journal:  RSC Adv       Date:  2020-06-08       Impact factor: 4.036

Review 9.  Recent development of multifunctional agents as potential drug candidates for the treatment of Alzheimer's disease.

Authors:  Natalia Guzior; Anna Wieckowska; Dawid Panek; Barbara Malawska
Journal:  Curr Med Chem       Date:  2015       Impact factor: 4.530

Review 10.  Advances in Multi-Functional Ligands and the Need for Metal-Related Pharmacology for the Management of Alzheimer Disease.

Authors:  Abha Sharma; Vidhu Pachauri; S J S Flora
Journal:  Front Pharmacol       Date:  2018-11-15       Impact factor: 5.810
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