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Molecules
Special Issues
Design, Synthesis, and Evaluations of Antidepressant/Anticonvulsant/Anti-Alzheimer Agents
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Design, Synthesis, and Evaluations of Antidepressant/Anticonvulsant/Anti-Alzheimer Agents

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (25 July 2023) | Viewed by 4321

Special Issue Editors

Dr. Liping Guan

E-Mail Website
Guest Editor
Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China
Interests: antidepressant; anti-Alzheimer’s disease; anti-convulsion; organic synthesis; lead compounds of antiepileptic and antidepressant drugs
Dr. Xianqing Deng

E-Mail Website
Guest Editor
Medical College, Jinggangshan University, Ji'an 343009, China
Interests: antidepressant; anticonvulsant; organic synthesis; anticancer; lead compounds of antiepileptic and antidepressant drugs

Special Issue Information

Dear Colleagues,

Neurologic disorders such as depression, convulsion, epilepsy, and Alzheimer’s disease affect many people. In recent years, we have witnessed the discovery of numerous new organic compounds as potential antidepressant/anticonvulsant/anti-Alzheimer agents from de novo synthesis or structural modification of natural products. However, the development of new candidate drugs for the treatment of these diseases is still an urgent and intense need. Hence, so many scientists around the world are still involved in the discovery of new substances with antidepressant/anticonvulsant/anti-Alzheimer's disease activity. 

The aim of this Special Issue is to provide a platform for all scientists who are currently engaged in antidepressant/anticonvulsant/anti-Alzheimer drugs research.

It is our great pleasure to invite you to contribute to this Special Issue and present your work in the form of communications, articles, or reviews.

Dr. Liping Guan
Dr. Xianqing Deng
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 submissions that pass pre-check are 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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). 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

  • monoamine oxidase
  • cholinesterase
  • synthesis
  • antidepressant
  • anti-Alzheimer's disease
  • anticonvulsant
  • antiepileptic
  • antiseizure

Published Papers (3 papers)

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Research

15 pages, 6909 KiB  
Article
Antiseizure Properties of Histamine H3 Receptor Antagonists Belonging 3,4-Dihydroquinolin-2(1H)-Ones
by Yi Hua, Mingxia Song, Qiaoyue Guo, Yiqin Luo, Xianqing Deng and Yushan Huang
Molecules 2023, 28(8), 3408; https://doi.org/10.3390/molecules28083408 - 12 Apr 2023
Cited by 1 | Viewed by 940
Abstract
H3R is becoming an attractive and promising target for epilepsy treatment as well as the discovery of antiepileptics. In this work, a series of 6-aminoalkoxy-3,4-dihydroquinolin-2(1H)-ones was prepared to screen their H3R antagonistic activities and antiseizure effects. The [...] Read more.
H3R is becoming an attractive and promising target for epilepsy treatment as well as the discovery of antiepileptics. In this work, a series of 6-aminoalkoxy-3,4-dihydroquinolin-2(1H)-ones was prepared to screen their H3R antagonistic activities and antiseizure effects. The majority of the target compounds displayed a potent H3R antagonistic activity. Among them, compounds 2a, 2c, 2h, and 4a showed submicromolar H3R antagonistic activity with an IC50 of 0.52, 0.47, 0.12, and 0.37 μM, respectively. The maximal electroshock seizure (MES) model screened out three compounds (2h, 4a, and 4b) with antiseizure activity. Meanwhile, the pentylenetetrazole (PTZ)-induced seizure test gave a result that no compound can resist the seizures induced by PTZ. Additionally, the anti-MES action of compound 4a fully vanished when it was administrated combined with an H3R agonist (RAMH). These results showed that the antiseizure role of compound 4a might be achieved by antagonizing the H3R receptor. The molecular docking of 2h, 4a, and PIT with the H3R protein predicted their possible binding patterns and gave a presentation that 2h, 4a, and PIT had a similar binding model with H3R. Full article
(This article belongs to the Special Issue Design, Synthesis, and Evaluations of Antidepressant/Anticonvulsant/Anti-Alzheimer Agents)
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16 pages, 2477 KiB  
Article
Design, Synthesis, and Pharmacology of New Triazole-Containing Quinolinones as CNS Active Agents
by Wennan Zhao, Mingxia Song, Yi Hua, Yangnv Zhu, Wenli Liu, Qishan Xia, Xianqing Deng and Yushan Huang
Molecules 2023, 28(4), 1987; https://doi.org/10.3390/molecules28041987 - 20 Feb 2023
Cited by 1 | Viewed by 1643
Abstract
Epilepsy and major depressive disorder are the two of the most common central nervous system (CNS) diseases. Clinicians and patients call for new antidepressants, antiseizure medicines, and in particular drugs for depression and epilepsy comorbidities. In this work, a dozen new triazole-quinolinones were [...] Read more.
Epilepsy and major depressive disorder are the two of the most common central nervous system (CNS) diseases. Clinicians and patients call for new antidepressants, antiseizure medicines, and in particular drugs for depression and epilepsy comorbidities. In this work, a dozen new triazole-quinolinones were designed, synthesized, and investigated as CNS active agents. All compounds reduced the immobility time significantly during the forced swim test (FST) in mice at the dosage of 50 mg/kg. Compounds 3f–3j gave superior performance over fluoxetine in the FST with more reductions of the immobility time. Compound 3g also reduced immobility time significantly in a tail suspension test (TST) at the dosage of 50 mg/kg, though its anti-immobility activity was inferior to that of fluoxetine. An open field test was carried out and it eliminated the false-positive possibility of 3g in the FST and TST, which complementarily supported the antidepressant activity of 3g. We also found that almost all compounds except 3k exhibited antiseizure activity in the maximal electroshock seizure (MES) model at 100 or 300 mg/kg. Compounds 3c, 3f, and 3g displayed the ED50 of 63.4, 78.9, and 84.9 mg/kg, and TD50 of 264.1, 253.5, and 439.9 mg/kg, respectively. ELISA assays proved that the mechanism for the antiseizure and antidepressant activities of compound 3g was via affecting the concentration of GABA in mice brain. The molecular docking study showed a good interaction between 3g and the amino acid residue of the GABAA receptor. Excellent drug-like properties and pharmacokinetic properties of compound 3a–l were also predicted by Discovery Studio. These findings provided a new skeleton to develop agents for the treatment of epilepsy and depression comorbidities. Full article
(This article belongs to the Special Issue Design, Synthesis, and Evaluations of Antidepressant/Anticonvulsant/Anti-Alzheimer Agents)
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17 pages, 2945 KiB  
Article
(S)-N-Benzyl-1-phenyl-3,4-dihydroisoqunoline-2(1H)-carboxamide Derivatives, Multi-Target Inhibitors of Monoamine Oxidase and Cholinesterase: Design, Synthesis, and Biological Activity
by Qing-Hao Jin, Li-Ping Zhang, Shan-Shan Zhang, Dai-Na Zhuang, Chu-Yu Zhang, Zhou-Jun Zheng and Li-Ping Guan
Molecules 2023, 28(4), 1654; https://doi.org/10.3390/molecules28041654 - 09 Feb 2023
Cited by 3 | Viewed by 1380
Abstract
A series of (S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives was synthesized and evaluated for inhibitory activity against monoamine oxidase (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). Four compounds (2i, 2p, 2t, and 2v) showed good inhibitory [...] Read more.
A series of (S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives was synthesized and evaluated for inhibitory activity against monoamine oxidase (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). Four compounds (2i, 2p, 2t, and 2v) showed good inhibitory activity against both MAO-A and MAO-B, and two compounds (2d and 2j) showed selective inhibitory activity against MAO-A, with IC50 values of 1.38 and 2.48 µM, respectively. None of the compounds showed inhibitory activity against AChE; however, 12 compounds showed inhibitory activity against BChE. None of the active compounds showed cytotoxicity against L929cells. Molecular docking revealed several important interactions between the active analogs and amino acid residues of the protein receptors. This research paves the way for further study aimed at designing MAO and ChE inhibitors for the treatment of depression and neurodegenerative disorders. Full article
(This article belongs to the Special Issue Design, Synthesis, and Evaluations of Antidepressant/Anticonvulsant/Anti-Alzheimer Agents)
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