Special Issue "Triazole and Derivatives in Medicinal Chemistry"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 15 February 2024 | Viewed by 832

Special Issue Editor

Department of Electronic Engineering, Universitat Rovira i Virgili, Tarragona, Spain
Interests: organic chemistry; organic synthesis; catalysis; medicinal chemistry; pharmacy

Special Issue Information

Dear Colleagues,

The development of modern medicinal chemistry has tightened the heterocycles with biological activities. Several derivatives of heterocyclic compounds have found applications in various medical fields. Triazole, a five-member heterocycle with 3 nitrogen and 2 carbon atoms, is a significant backbone in medicinal chemistry. This backbone could be found in the structure of many commercial drugs. Since it is readily available through click chemistry to create compound collections against various diseases, it has become an emerging area of interest for medicinal chemists. As is widely known, triazole is the building block for numerous drugs with therapeutic benefits, including antimicrobial, antiviral, anticancer, anti-inflammatory, analgesic, anti-tuberculosis, and antidiabetic activities. In addition, this compound can form complexes with different compounds to form materials with catalytic and biological activities. Regarding the significance of this heterocycle, several researchers have focused on the synthesis of novel compounds based on triazoles and studying their biological activities. Although research efforts are focusing on the development of synthetic triazole analogs, there is still plenty of room for a breakthrough in drug discovery in this field. The potential therapeutic benefits of this moiety have motivated medicinal chemists to create innovative triazole derivatives.

This Special Issue of Pharmaceuticals focuses on "Triazole and Derivatives in Medicinal Chemistry” and invites both reviews and original articles regarding their findings in this field.

I look forward to receiving your contributions.

Dr. Saeed Bahadorikhalili
Guest Editor

Manuscript Submission Information

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Keywords

  • triazole
  • heterocycles
  • medicinal chemistry
  • pharmaceutical chemistry
  • organic synthesis
  • catalytic organic synthesis
  • bioactivity
  • organocatalysis

Published Papers (1 paper)

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Research

14 pages, 3301 KiB  
Article
Self-Assembling Polymers with p-Aminosalicylate Anions Supported by Encapsulation of p-Aminosalicylate for the Improvement of Drug Content and Release Efficiency
Pharmaceuticals 2023, 16(10), 1502; https://doi.org/10.3390/ph16101502 - 23 Oct 2023
Viewed by 549
Abstract
Bioactive linear choline-based copolymers were developed as micellar carriers for drug delivery systems (DDSs). The polymethacrylates containing trimethylammonium groups with p-aminosalicylate anions (PAS-based copolymers: series 1) or chloride anions (Cl-based copolymers: series 2) differing in ionic content and chain length were selected [...] Read more.
Bioactive linear choline-based copolymers were developed as micellar carriers for drug delivery systems (DDSs). The polymethacrylates containing trimethylammonium groups with p-aminosalicylate anions (PAS-based copolymers: series 1) or chloride anions (Cl-based copolymers: series 2) differing in ionic content and chain length were selected for drug loading. The diverse structures of amphiphilic copolymers made it possible to adjust the encapsulation efficiency of a well-known antibiotic, i.e., p-aminosalicylate in the form of sodium salt (PASNa) or acid (PASA), providing single drug systems. Goniometry was applied to verify the self-assembly capacity of the copolymers using the critical micelle concentration (CMC = 0.03–0.18 mg/mL) and the hydrophilicity level quantifying the surface wettability of polymer film using the water contact angle (WCA = 30–53°). Both parameters were regulated by the copolymer composition, indicating that the increase in ionic content caused higher CMC and lower WCA, but the latter was also modified to a less hydrophilic surface by drug encapsulation. The drug content (DC) in the PAS-based polymers was increased twice by encapsulation of PASNa and PASA (47–96% and 86–104%), whereas in the chloride-based polymer systems, the drug was loaded in 43–96% and 73–100%, respectively. Efficient drug release was detected for PASNa (80–100% series 1; 50–100% series 2) and PASA as complete in both series. The strategy of loading extra drug by encapsulation, which enhances the drug content in the copolymers containing anions of the same pharmaceutics, provided promising characteristics, which highlight the potential of PAS-loaded micellar copolymers for drug delivery. Full article
(This article belongs to the Special Issue Triazole and Derivatives in Medicinal Chemistry)
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