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Trends of Drug Synthesis in Medicinal Chemistry
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Trends of Drug Synthesis in Medicinal Chemistry

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

Deadline for manuscript submissions: 31 March 2026 | Viewed by 1016

Special Issue Editor

Dr. Cheng-Hua Jin

E-Mail Website
Guest Editor
1. College of Pharmacy, Yanbian University, Yanji 133002, China
2. Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University, Yanji 133002, China
Interests: synthetic pharmaceutical chemistry; antitumor drugs; antifibrotic drugs; natural products; antibacterial agents

Special Issue Information

Dear Colleagues,

This Special Issue highlights cutting-edge advances in synthetic methodologies across anticancer, antimicrobial, antiviral, anti-inflammatory, cardiovascular, and endocrine therapeutics. With the rise of targeted drug design, green chemistry, and AI platforms redefine oncology treatment, novel small-molecule protease inhibitors combat drug-resistant pathogens, and continuous-flow systems enhance scalable production. We invite contributions exploring catalytic asymmetric synthesis, bioorthogonal chemistry, and computational modeling applications, emphasizing their roles in improving drug efficacy, sustainability, and clinical translation. This collection aims to bridge interdisciplinary insights from organic chemistry, pharmacology, and engineering, fostering discussions on next-generation synthesis paradigms for global health challenges.

Dr. Cheng-Hua Jin
Guest Editor

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

  • drug synthesis
  • anticancer agents
  • antimicrobial resistance
  • green chemistry
  • AI-driven design
  • targeted delivery systems
  • continuous-flow technology
  • structure–activity optimization
  • multidisciplinary collaboration

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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Research

18 pages, 2985 KB  
Article
Multicomponent Synthesis of Multi-Target Quinazolines Modulating Cholinesterase, Oxidative Stress, and Amyloid Aggregation Activities for the Therapy of Alzheimer’s Disease
by Saida Chakhari, José Marco-Contelles, Isabel Iriepa, Maria do Carmo Carreiras, Fakher Chabchoub, Lhassane Ismaili and Bernard Refouvelet
Molecules 2025, 30(19), 3930; https://doi.org/10.3390/molecules30193930 - 30 Sep 2025
Abstract
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder characterized by extracellular accumulation of amyloid-beta (Aβ) peptide, intracellular neurofibrillary tangles (NFTs), severe neuronal loss, and a marked decline in cholinergic function. Due to the limited efficacy of currently available therapies, the search for new [...] Read more.
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder characterized by extracellular accumulation of amyloid-beta (Aβ) peptide, intracellular neurofibrillary tangles (NFTs), severe neuronal loss, and a marked decline in cholinergic function. Due to the limited efficacy of currently available therapies, the search for new chemical scaffolds able to target multiple pathological mechanisms remains an urgent priority. Among the most promising strategies are heterocyclic frameworks that can simultaneously interact with cholinesterase (ChE) enzymes and inhibit amyloid-β (Aβ) aggregation while also exhibiting antioxidant activity. In this context, we report a series of quinazoline derivatives synthesized via a sequential, one-pot multicomponent reaction, in good yields. Several of these compounds demonstrated notable antioxidant properties, as well as inhibitory effects on ChE activity and Aβ1-42 self-aggregation, highlighting their potential as multifunctional agents for the treatment of neurodegenerative disorders. Notably, 2-ethyl-4-(3,4-Dimethoxyphenyl)aminoquinazoline (3h) demonstrated the most balanced biological profile among the tested compounds, exhibiting an ORAC value of 5.73 TE, an acetylcholinesterase (AChE) inhibition IC50 = 6.67 μM, and 36.68% inhibition of Aβ1–42 aggregation, closely approaching the activity of curcumin. These findings highlight compound 3h as a promising quinazoline-based hit for the development of multifunctional agents targeting AD. Full article
(This article belongs to the Special Issue Trends of Drug Synthesis in Medicinal Chemistry)
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28 pages, 1957 KB  
Article
Design and Synthesis of Sulfonium and Selenonium Derivatives Bearing 3′,5′-O-Benzylidene Acetal Side Chain Structure as Potent α-Glucosidase Inhibitors
by Xiaosong He, Jiahao Yi, Jianchen Yang, Genzoh Tanabe, Osamu Muraoka and Weijia Xie
Molecules 2025, 30(13), 2856; https://doi.org/10.3390/molecules30132856 - 4 Jul 2025
Viewed by 557
Abstract
A group of sulfonium and selenonium salts bearing diverse benzylidene acetal substituents on their side chain moiety were designed and synthesized. Compared with our previous study, structural modifications in this study focused on multi-substitution of the phenyl ring and bioisosteric replacements at the [...] Read more.
A group of sulfonium and selenonium salts bearing diverse benzylidene acetal substituents on their side chain moiety were designed and synthesized. Compared with our previous study, structural modifications in this study focused on multi-substitution of the phenyl ring and bioisosteric replacements at the sulfonium cation center. In vitro biological evaluation showed that selenonium replacement could significantly improve their α-glucosidase inhibitory activity. The most potent inhibitor 20c (10.0 mg/kg) reduced postprandial blood glucose by 48.6% (15 min), 52.8% (30 min), and 48.1% (60 min) in sucrose-loaded mice, outperforming acarbose (20.0 mg/kg). Docking studies of 20c with ntMGAM presented a new binding mode. In addition to conventional hydrogen bonding and electrostatic interaction, amino residue Ala-576 was first identified to contribute to binding affinity through π-alkyl and alkyl interactions with the chlorinated substituent and aromatic ring. The selected compounds exhibited a high degree of safety in cytotoxicity tests against normal cells. Kinetic characterization of α-glucosidase inhibition confirmed a fully competitive inhibitory mode of action for these sulfonium salts. Full article
(This article belongs to the Special Issue Trends of Drug Synthesis in Medicinal Chemistry)
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