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Synthesis, Characterization and Biological Activity of Pharmaceutically Important Drug Molecules

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

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 1757

Special Issue Editors


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Guest Editor
Division of Sustainable Agriculture, The Energy and Resources Institute, Gwal Pahari, Gurugram, Haryana 122003, India
Interests: drug delivery; drug molecules; biological activities; synthesis; characterization; anti-cancer; natural products; sensing
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The drug discovery process is a challenging multi-step path towards the identification of potential new medicines. The driving force of this process is an unmet medical need for new drugs to prevent disease, fight pathology, or diagnose medical conditions for which there are currently no suitable medical products. There is an ongoing intensive search for drug-like molecules that can be obtained via chemical synthesis from smaller chemical building blocks or isolated from natural sources such as plants. Currently, the drugs on the market are of both natural and synthetic origin; however, there are also semi-synthetic drugs, which are generally obtained by converting starting materials from natural sources into final products via chemical reactions. This Special Issue will publish papers that describe the synthesis, characterization, and biological activity of important synthetic, semi-synthetic, and natural drug molecules. We welcome research articles, as well as those describing cytotoxic chemical libraries that include bioactive compounds/molecules with novel substitution patterns. Given the recent developments in drug design and organic and inorganic chemistry, review articles on these topics will also be considered.

Dr. Vivek K. Bajpai
Dr. Shruti Shukla
Guest Editors

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Keywords

  • synthesis 
  • characterization 
  • biological activities 
  • bioactive drug molecules 
  • drug delivery

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Published Papers (1 paper)

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Research

14 pages, 3971 KiB  
Article
Oxidation of Mesalamine under Phenoloxidase- or Peroxidase-like Enzyme Catalysis
by Rimaz El Zein, Pompilia Ispas-Szabo, Maziar Jafari, Mohamed Siaj and Mircea Alexandru Mateescu
Molecules 2023, 28(24), 8105; https://doi.org/10.3390/molecules28248105 - 15 Dec 2023
Viewed by 1403
Abstract
Mesalamine, also called 5-ASA (5-aminosalicylic acid), is a largely used anti-inflammatory agent and is a main choice to treat Ulcerative Colitis. This report is aimed to investigate enzymatic processes involved in the oxidation of mesalamine to better understand some of its side-effects. Oxidation [...] Read more.
Mesalamine, also called 5-ASA (5-aminosalicylic acid), is a largely used anti-inflammatory agent and is a main choice to treat Ulcerative Colitis. This report is aimed to investigate enzymatic processes involved in the oxidation of mesalamine to better understand some of its side-effects. Oxidation with oxygen (catalyzed by ceruloplasmin) or with hydrogen peroxide (catalyzed by peroxidase or hemoglobin) showed that these oxidases, despite their different mechanisms of oxidation, could recognize mesalamine as a substrate and trigger its oxidation to a corresponding quinone-imine. These enzymes were chosen because they may recognize hydroquinone (a p-diphenol) as substrate and oxidize it to p-benzoquinone and that mesalamine, as a p-aminophenol, presents some similarities with hydroquinone. The UV-Vis kinetics, FTIR and 1H NMR supported the hypothesis of oxidizing mesalamine. Furthermore, mass spectrometry suggested the quinone–imine as reaction product. Without enzymes, the oxidation process was very slow (days and weeks), but it was markedly accelerated with the oxidases, particularly with peroxidase. Cyclic voltammetry supported the hypothesis of the oxidative process and allowed a ranking of susceptibility to oxidizing mesalamine in comparison with other oxidizable drug molecules with related structures. The susceptibility to oxidation was higher for mesalamine, in comparison with Tylenol (acetaminophen) and with aspirin (salicylic acid). Full article
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