Prodrugs and Molecular Hybrids as Innovative Strategies in Medicinal Chemistry

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (10 June 2024) | Viewed by 3105

Special Issue Editors


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Guest Editor
Department of Drug Science and Technology, University of Turin, 10125 Turin, Italy
Interests: nitric oxide; NO-(photo)donors; molecular hybrid strategy; prodrug strategy; drug discovery; drug development
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
1. Department of Pharmacy, University of Napoli Federico II, 80131 Napoli, Italy
2. Department of Drug Science and Technology, University of Turin, 10125 Turin, Italy
Interests: NO-(photo)donors; prodrug strategy; carbohydrate-based prodrugs; molecular hybrid design; drug design; drug delivery; drug targeting
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmacy, University of Napoli Federico II, 80131 Napoli, Italy
Interests: prodrug strategy; carbohydrate-based prodrugs; drug targeting; drug discovery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Prodrug Design is a well-known strategy of chemically modifying the structure of a drug, which is called the "parent drug." This approach makes it possible to optimize the physiochemical and pharmacological properties of a parent drug, resulting in improvement of its pharmacokinetic characteristics and reduction of its toxicity.

Another innovative strategy used in medicinal chemistry is Molecular Hybridization. This is a new drug design and development concept based on combining pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy compared with parent drugs. In addition, this approach can lead to compounds with a modified selectivity profile, different and/or dual modes of action, and reduced unwanted side effects.

In this Special Issue "Prodrugs and Molecular Hybrids as Innovative Strategies in Medicinal Chemistry", we aim to collect both original articles and up-to-date reviews that focus on the design, synthesis, physiochemical and biological characterization of novel prodrugs and/or molecular hybrids that have been shown to overcome many limitations related to the pharmaceutical, pharmacokinetics and/or pharmacodynamics phase of the parent drugs.

As Guest Editor, we encourage researchers working in this area to contribute their recent studies to this Special Issue of Pharmaceutics.

Prof. Dr. Loretta Lazzarato
Dr. Sodano Federica
Prof. Dr. Maria Grazia Rimoli
Guest Editors

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Keywords

  • prodrugs
  • bioprecursors
  • carrier prodrugs
  • macromolecular prodrugs
  • mutual prodrugs
  • molecular hybrids
  • hybrid drugs
  • macromolecular hybrids
  • anti-inflammatory activity
  • antimicrobial activity
  • anticancer activity
  • biomedical applications
  • physicochemical characterization
  • pharmacokinetics profile
  • pharmacodynamics properties
  • drug targeting
  • drug delivery
  • drug discovery
  • drug development
  • toxicity

Published Papers (2 papers)

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Research

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14 pages, 1795 KiB  
Article
N-Succinylaspartic-Acid-Conjugated Riluzole Is a Safe and Potent Colon-Targeted Prodrug of Riluzole against DNBS-Induced Rat Colitis
by Jaejeong Kim, Changyu Kang, Jin-Wook Yoo, In-Soo Yoon and Yunjin Jung
Pharmaceutics 2023, 15(11), 2638; https://doi.org/10.3390/pharmaceutics15112638 - 16 Nov 2023
Cited by 1 | Viewed by 1009
Abstract
In our previous study, riluzole azo-linked to salicylic acid (RAS) was prepared as a colon-targeted prodrug of riluzole (RLZ) to facilitate the repositioning of RLZ as an anticolitic drug. RAS is more effective against rat colitis than RLZ and sulfasalazine, currently used as [...] Read more.
In our previous study, riluzole azo-linked to salicylic acid (RAS) was prepared as a colon-targeted prodrug of riluzole (RLZ) to facilitate the repositioning of RLZ as an anticolitic drug. RAS is more effective against rat colitis than RLZ and sulfasalazine, currently used as an anti-inflammatory bowel disease drug. The aim of this study is to further improve colon specificity, anticolitic potency, and safety of RAS. N-succinylaspart-1-ylRLZ (SAR) and N-succinylglutam-1-ylRLZ (SGR) were synthesized and evaluated as a “me-better” colon-targeted prodrug of RLZ against rat colitis. SAR but not SGR was converted to RLZ in the cecal contents, whereas both conjugates remained intact in the small intestine. When comparing the colon specificity of SAR with that of RAS, the distribution coefficient and cell permeability of SAR were lower than those of RAS. In parallel, oral SAR delivered a greater amount of RLZ to the cecum of rats than oral RAS. In a DNBS-induced rat model of colitis, oral SAR mitigated colonic damage and inflammation and was more potent than oral RAS. Moreover, upon oral administration, SAR had a greater ability to limit the systemic absorption of RLZ than RAS, indicating a reduced risk of systemic side effects of SAR. Taken together, SAR may be a “me-better” colon-targeted prodrug of RLZ to improve the safety and anticolitic potency of RAS, an azo-type colon-targeted prodrug of RLZ. Full article
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Review

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54 pages, 14655 KiB  
Review
An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)
by Daniel Ungureanu, Brîndușa Tiperciuc, Cristina Nastasă, Ioana Ionuț, Gabriel Marc, Ilioara Oniga and Ovidiu Oniga
Pharmaceutics 2024, 16(1), 89; https://doi.org/10.3390/pharmaceutics16010089 - 9 Jan 2024
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Abstract
Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue is the synthesis of novel antimicrobials through rational drug design based on extensive structure–activity relationship studies. The thiazole nucleus is a prominent feature in the [...] Read more.
Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue is the synthesis of novel antimicrobials through rational drug design based on extensive structure–activity relationship studies. The thiazole nucleus is a prominent feature in the structure of many authorized antimicrobials, being clubbed with different heterocycles. The purpose of this review is to study the structure–activity relationship in antimicrobial thiazoles clubbed with various heterocycles, as reported in the literature between 2017 and 2023, in order to offer an overview of the last years in terms of antimicrobial research and provide a helpful instrument for future research in the field. Full article
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