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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: 30 September 2025 | Viewed by 372

Special Issue Editor


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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

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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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Published Papers (1 paper)

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Research

28 pages, 1957 KiB  
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 261
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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