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Organic Molecules in Drug Discovery and Development

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

Deadline for manuscript submissions: 31 July 2025 | Viewed by 744

Special Issue Editor


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Guest Editor
Department of Chemistry, University of Patras, 26504 Patras, Greece
Interests: organic synthesis; medicinal chemistry; drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Organic Chemistry and Organic Synthesis in Drug Discovery and Development plays a significant role in both the synthesis of bioactive compounds for further investigation, as well as the development of synthetic approaches that combine creativity and innovation regarding the application of organic chemistry in drug development.

This Special Issue will collect full papers, communication papers, and review articles that address all stages of drug discovery and development, from target identification and validation to preclinical evaluation; this includes innovative methodologies and optimization strategies for the synthesis of organic molecules with potential pharmaceutical interest. In addition to small organic molecules, this Special Issue will also address the chemistry of peptides and modified peptide molecules, bioconjugates and other types of macromolecules of potential pharmaceutical interest.

Dr. Spyridon Mourtas
Guest Editor

Manuscript Submission Information

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Keywords

  • organic chemistry
  • chemical synthesis
  • chemical modifications
  • organic molecules
  • molecular mechanisms
  • bioactivity
  • drug development
  • drugs

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Published Papers (1 paper)

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Research

15 pages, 779 KiB  
Article
Balancing Yields and Sustainability: An Eco-Friendly Approach to Losartan Synthesis Using Green Palladium Nanoparticles
by Edith M. Antunes, Yusuf A. Adegoke, Sinazo Mgwigwi, John J. Bolton, Sarel F. Malan and Denzil R. Beukes
Molecules 2025, 30(11), 2314; https://doi.org/10.3390/molecules30112314 - 25 May 2025
Viewed by 323
Abstract
This study presents a sustainable, environmentally friendly synthetic route for the production of key intermediates in losartan using palladium nanoparticles (PdNPs) derived from a brown seaweed, Sargassum incisifolium, as a recyclable nanocatalyst. A key intermediate, biaryl, was synthesized with an excellent yield [...] Read more.
This study presents a sustainable, environmentally friendly synthetic route for the production of key intermediates in losartan using palladium nanoparticles (PdNPs) derived from a brown seaweed, Sargassum incisifolium, as a recyclable nanocatalyst. A key intermediate, biaryl, was synthesized with an excellent yield (98%) via Suzuki–Miyaura coupling between 2-bromobenzonitrile and 4-methylphenylboronic acid, catalyzed using bio-derived PdNPs under mild conditions. Subsequent bromination using N-bromosuccinimide (NBS) under LED light, followed by imidazole coupling and tetrazole ring formation, allowed for the production of losartan with an overall yield of 27%. The PdNP catalyst exhibited high stability and recyclability, as well as strong catalytic activity, even at lower loadings, and nitrosamine formation was not detected. While the overall yield was lower than that of traditional industrial methods, this was due to the deliberate avoidance of the use of toxic reagents, hazardous solvents, and protection/deprotection steps commonly used in conventional routes. This trade-off marks a shift in pharmaceutical process development, where environmental and safety considerations are increasingly prioritized in line with green chemistry and regulatory frameworks. This study provides a foundation for green scaling up strategies, incorporating sustainability principles into drug synthesis. Full article
(This article belongs to the Special Issue Organic Molecules in Drug Discovery and Development)
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