The impact of wingtip N-substitution on the bioactivity of azolium salts.
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| Title: | The impact of wingtip N-substitution on the bioactivity of azolium salts. |
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| Authors: | Ibrahim H; Department of Chemistry, Durban University of Technology, P.O Box 1334, Durban, 4000, South Africa., Bala MD; School of Chemistry and Physics, University of KwaZulu Natal, Private Bag X54001, Durban, 4000, South Africa. Electronic address: bala@ukzn.ac.za., Ntola P; Department of Chemistry, Durban University of Technology, P.O Box 1334, Durban, 4000, South Africa. |
| Source: | European journal of medicinal chemistry [Eur J Med Chem] 2025 Oct 05; Vol. 295, pp. 117797. Date of Electronic Publication: 2025 May 27. |
| Publication Type: | Journal Article; Review |
| Language: | English |
| Journal Info: | Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE |
| Imprint Name(s): | Publication: Paris : Editions Scientifiques Elsevier Original Publication: Paris, S.E.C.T. [etc.] |
| MeSH Terms: | Azo Compounds*/chemistry , Azo Compounds*/pharmacology, Animals ; Humans ; Molecular Structure ; Salts/chemistry ; Salts/pharmacology ; Structure-Activity Relationship ; Triazoles/chemistry ; Triazoles/pharmacology |
| Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. Studies have shown that the physicochemical properties of five-membered heterocyclic azolium compounds directly affect their biological activity as therapeutic drugs (spectrum of activity and potency) and the associated pharmacokinetic, pharmacologic, and toxicological profiles of the compounds. Hence, this review focused on the influence of N-functionalisation at the wingtip of such compounds, mainly the diazolium and the triazolium-based salts. The contribution of the N-donor groups to the overall biological efficacy of the azolium compounds and the ensuing structure-activity mechanisms in their pharmacological applications are comprehensively discussed. (Copyright © 2025 The Authors. Published by Elsevier Masson SAS.. All rights reserved.) |
| Contributed Indexing: | Keywords: Antitumour; Benzimidazolium; Imidazolium; N-functionalisation; antimicrobial; molecular structure; triazolium |
| Substance Nomenclature: | 0 (Azo Compounds) 0 (Salts) 0 (Triazoles) |
| Entry Date(s): | Date Created: 20250531 Date Completed: 20250608 Latest Revision: 20250609 |
| Update Code: | 20250609 |
| DOI: | 10.1016/j.ejmech.2025.117797 |
| PMID: | 40449118 |
| Database: | MEDLINE |
| Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br />Studies have shown that the physicochemical properties of five-membered heterocyclic azolium compounds directly affect their biological activity as therapeutic drugs (spectrum of activity and potency) and the associated pharmacokinetic, pharmacologic, and toxicological profiles of the compounds. Hence, this review focused on the influence of N-functionalisation at the wingtip of such compounds, mainly the diazolium and the triazolium-based salts. The contribution of the N-donor groups to the overall biological efficacy of the azolium compounds and the ensuing structure-activity mechanisms in their pharmacological applications are comprehensively discussed.<br /> (Copyright © 2025 The Authors. Published by Elsevier Masson SAS.. All rights reserved.) |
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| ISSN: | 1768-3254 |
| DOI: | 10.1016/j.ejmech.2025.117797 |
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