The Role of Five-Membered Heterocycles in the Molecular Structure of Antibacterial Drugs Used in Therapy
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Published:2023-10-29
Issue:11
Volume:15
Page:2554
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ISSN:1999-4923
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Container-title:Pharmaceutics
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language:en
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Short-container-title:Pharmaceutics
Author:
Rusu Aura1ORCID, Moga Ioana-Maria1ORCID, Uncu Livia2ORCID, Hancu Gabriel1ORCID
Affiliation:
1. Pharmaceutical and Therapeutic Chemistry Department, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science and Technology of Targu Mures, 540142 Targu Mures, Romania 2. Scientific Center for Drug Research, “Nicolae Testemitanu” State University of Medicine and Pharmacy, 8 Bd. Stefan Cel Mare si Sfant 165, MD-2004 Chisinau, Moldova
Abstract
Five-membered heterocycles are essential structural components in various antibacterial drugs; the physicochemical properties of a five-membered heterocycle can play a crucial role in determining the biological activity of an antibacterial drug. These properties can affect the drug’s activity spectrum, potency, and pharmacokinetic and toxicological properties. Using scientific databases, we identified and discussed the antibacterials used in therapy, containing five-membered heterocycles in their molecular structure. The identified five-membered heterocycles used in antibacterial design contain one to four heteroatoms (nitrogen, oxygen, and sulfur). Antibacterials containing five-membered heterocycles were discussed, highlighting the biological properties imprinted by the targeted heterocycle. In some antibacterials, heterocycles with five atoms are pharmacophores responsible for their specific antibacterial activity. As pharmacophores, these heterocycles help design new medicinal molecules, improving their potency and selectivity and comprehending the structure-activity relationship of antibiotics. Unfortunately, particular heterocycles can also affect the drug’s potential toxicity. The review extensively presents the most successful five-atom heterocycles used to design antibacterial essential medicines. Understanding and optimizing the intrinsic characteristics of a five-membered heterocycle can help the development of antibacterial drugs with improved activity, pharmacokinetic profile, and safety.
Subject
Pharmaceutical Science
Reference195 articles.
1. Gupta, R.R., Kumar, M., and Gupta, V. (2013). Heterocyclic Chemistry: Volume II: Five-Membered Heterocycles, Springer Science & Business Media. 2. Heterocycles in Drugs and Drug Discovery;Gomtsyan;Chem. Heterocycl. Comp.,2012 3. Identification of Pyrrolo [3′,4′:3,4]Cyclohepta[1,2-d][1,2]Oxazoles as Promising New Candidates for the Treatment of Lymphomas;Barreca;Eur. J. Med. Chem.,2023 4. Grillone, K., Riillo, C., Rocca, R., Ascrizzi, S., Spanò, V., Scionti, F., Polerà, N., Maruca, A., Barreca, M., and Juli, G. (2022). The New Microtubule-Targeting Agent SIX2G Induces Immunogenic Cell Death in Multiple Myeloma. Int. J. Mol. Sci., 23. 5. Synthesis and Discovery of the First Potent Proteolysis Targeting Chimaera (PROTAC) Degrader of AIMP2-DX2 as a Lung Cancer Drug;Lee;J. Enzym. Inhib. Med. Chem.,2023
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