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Special Issue "Newly Developed Drugs for Alzheimer's Disease"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Neurobiology".

Deadline for manuscript submissions: 30 September 2021.

Special Issue Editors

Prof. Dr. Kamil Kuca
E-Mail Website1 Website2 Website3 Website4
Guest Editor
Department of Chemistry, Faculty of Science, University of Hradec Kralove, Hradec Kralove, Czech Republic
Biomedical Research Center, University Hospital Hradec Kralove, Hradec Kralove, Czech Republic
Interests: drug design and development; antidotes for pesticide and nerve agent intoxications; Alzheimer’s disease; detergents as disinfectants, decontamination means; toxins; nanotechnology; project management; scientific management; technology transfer; health economics and pharmacoeconomics
Special Issues and Collections in MDPI journals
Dr. Martin Valis
E-Mail Website
Guest Editor
Neurology Clinic, University Hospital Hradec Kralove, Hradec Kralove, Czech Republic
Interests: brain damage; neurology; Alzheimer’s disease
Special Issues and Collections in MDPI journals
Dr. Eugenie Nepovimova
E-Mail Website
Guest Editor
Department of Chemistry, Faculty of Science, University of Hradec Kralove, Hradec Kralove, Czech Republic
Interests: Alzheimer’s disease; Antiaging drugs; Nerve agent antidotes
Special Issues and Collections in MDPI journals

Special Issue Information

Dear Colleagues,

Searching for novel drugs for the treatment of Alzheimer’s disease (AD) has become a main task of current developed societies. There novel drug candidates were/are and will be designed, synthesized and tested in many parts of the world. Despite tremendous advances in the understanding of many aspects of AD pathogenesis, there are no proven disease-modifying therapies, and the only available ones are minimally effective symptomatic therapies.

AD is associated with an enzyme acetylcholinesterase (AChE), which is a target for the development of novel drug candidates for these diseases.

In this Special Issue of International Journal of Molecular Sciences, we would like to discuss all chemico-biological aspects are behind Alzheimer’s disease, and related diseases.

Prof. Dr. Kamil Kuca
Dr. Martin Valis
Dr. Eugenie Nepovimova
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • alzheimer’s disease
  • drug development
  • therapy
  • treatment
  • biomarkers
  • pathophysiology
  • mechanism
  • novel drugs
  • preclinical
  • drug candidate

Published Papers (1 paper)

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Research

Open AccessArticle
Synthesis of New Biscoumarin Derivatives, In Vitro Cholinesterase Inhibition, Molecular Modelling and Antiproliferative Effect in A549 Human Lung Carcinoma Cells
Int. J. Mol. Sci. 2021, 22(8), 3830; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22083830 - 07 Apr 2021
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Abstract
A series of novel C4-C7-tethered biscoumarin derivatives (12ae) linked through piperazine moiety was designed, synthesized, and evaluated biological/therapeutic potential. Biscoumarin 12d was found to be the most effective inhibitor of both acetylcholinesterase (AChE, IC50 = 6.30 µM) and [...] Read more.
A series of novel C4-C7-tethered biscoumarin derivatives (12ae) linked through piperazine moiety was designed, synthesized, and evaluated biological/therapeutic potential. Biscoumarin 12d was found to be the most effective inhibitor of both acetylcholinesterase (AChE, IC50 = 6.30 µM) and butyrylcholinesterase (BChE, IC50 = 49 µM). Detailed molecular modelling studies compared the accommodation of ensaculin (well-established coumarin derivative tested in phase I of clinical trials) and 12d in the human recombinant AChE (hAChE) active site. The ability of novel compounds to cross the blood–brain barrier (BBB) was predicted with a positive outcome for compound 12e. The antiproliferative effects of newly synthesized biscoumarin derivatives were tested in vitro on human lung carcinoma cell line (A549) and normal colon fibroblast cell line (CCD-18Co). The effect of derivatives on cell proliferation was evaluated by MTT assay, quantification of cell numbers and viability, colony-forming assay, analysis of cell cycle distribution and mitotic activity. Intracellular localization of used derivatives in A549 cells was confirmed by confocal microscopy. Derivatives 12d and 12e showed significant antiproliferative activity in A549 cancer cells without a significant effect on normal CCD-18Co cells. The inhibition of hAChE/human recombinant BChE (hBChE), the antiproliferative activity on cancer cells, and the ability to cross the BBB suggest the high potential of biscoumarin derivatives. Beside the treatment of cancer, 12e might be applicable against disorders such as schizophrenia, and 12d could serve future development as therapeutic agents in the prevention and/or treatment of Alzheimer’s disease. Full article
(This article belongs to the Special Issue Newly Developed Drugs for Alzheimer's Disease)
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