In the last decades fungal infections became a major threat to human health having an unacceptably occurrence, a high rate of mortality and the number of patients at risk for these infections continue to increase every year. An effective, modern and very useful strategy in antifungal therapy is represented by the use of chimeric and hybrid drugs, most of them being with azaheterocycle skeleton. In this review, we present an overview from the last five years of the most representative achievements in the field of chimeric and hybrid diazine derivatives with antifungal properties. Within this work we emphasize the most relevant data concerning the synthesis, design, Structure Activity Relationships (SAR) correlations and antifungal activity of the main classes of diazine: 1,2-diazine (pyridazine), 1,3-diazine (pyrimidine), 1,4-diazine (pyrazine) and their fused derivatives.
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http://dx.doi.org/10.1016/j.bmc.2025.118069 | DOI Listing |
Bioorg Med Chem
January 2025
Alexandru Ioan Cuza University of Iasi, Faculty of Chemistry, Bd. Carol 11, 700506 Iasi, Romania. Electronic address:
In the last decades fungal infections became a major threat to human health having an unacceptably occurrence, a high rate of mortality and the number of patients at risk for these infections continue to increase every year. An effective, modern and very useful strategy in antifungal therapy is represented by the use of chimeric and hybrid drugs, most of them being with azaheterocycle skeleton. In this review, we present an overview from the last five years of the most representative achievements in the field of chimeric and hybrid diazine derivatives with antifungal properties.
View Article and Find Full Text PDFChem Biodivers
December 2024
Department of Food Science, Faculty of Food Science and Technology, Universiti Putra Malaysia, Selangor, Malaysia.
The UHPLC-MS/MS metabolomics approach was employed to profile and characterize multi-components in Halamphora sp. extracted with different solvents that contribute to quorum sensing inhibitory (QSI) activity. A total of 37 and 34 metabolites were tentatively identified from negative and positive ion modes, respectively.
View Article and Find Full Text PDFActa Crystallogr C Struct Chem
August 2024
University of Lodz, Faculty of Chemistry, Department of Physical Chemistry, Pomorska 163/165, 90-236 Lodz, Poland.
Cocrystals of thiourea with pyrazine N-oxide as thiourea-pyrazine N-oxide (2/1), CHNO·2CHNS, (I), and with phenazine as thiourea-phenazine (6/7), 7CHN·6CHNS, (II), both crystallize in the monoclinic space group P2/c. In the crystalline state, molecules of both components are linked by N-H..
View Article and Find Full Text PDFJ Agric Food Chem
July 2024
Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran 1417614411, Iran.
With fungal diseases posing a major threat to agricultural production, the application of fungicides to control related diseases is often considered necessary to ensure the world's food supply. The search for new bioactive agents has long been a priority in crop protection due to the continuous development of resistance against currently used types of active compounds. Heterocyclic compounds are an inseparable part of the core structures of numerous lead compounds, these rings constitute pharmacophores of a significant number of fungicides developed over the past decade by agrochemists.
View Article and Find Full Text PDFJ Am Chem Soc
May 2024
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, Florida 32611, United States.
Despite much progress in the area of dearomatization, the enantioselective dearomatization of heterocycles is limited to those with a single heteroatom. Here we report a highly enantioselective copper-catalyzed dearomatization of pyrazine, a diazine, leading to chiral C-substituted piperazines. When exposed to a chloroformate and an alkyne in the presence of a catalyst derived from a copper salt and the chiral ligand StackPhos, pyrazine is readily dearomatized to provide a 2,3-disubstituted dihydropyrazine as single diastereomer in high enantiomeric excess.
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