The aim of this study was to formulate and evaluate an experimental adhesive resin with the addition of 1,3,5-triacryloylhexahydro-1,3,5-triazine at different concentrations. Experimental adhesive resins were obtained by mixing 50% wt bisphenol A glycol dimethacrylate (BisGMA), 25% wt triethylene glycol dimethacrylate (TEGDMA), 25% wt 2-hydroxyethyl methacrylate (HEMA) and photoinitiator system. The triazine compound was added in 1, 2.5 and 5% wt to a base adhesive resin and one group remained with no triazine as control group. The experimental adhesive resins were analyzed for antibacterial activity (n=3), degree of conversion (n=3) and softening in solvent (n=3). Data distribution was evaluated by Kolmogorov-Smirnov test, paired t test, one-way ANOVA and Tukey's with a 0.05 level of significance. All groups with added triazine compound showed antibacterial activity against Streptococcus mutans (p<0.05). All groups achieved more than 70% degree of conversion, but there was no difference in this chemical property (p>0.05). The initial Knoop hardness was higher in 2.5 and 5% wt groups (p<0.05) and both groups present lower percentage variation of Knoop hardness after solvent degradation. The present study formulated an antibacterial adhesive resin with a non-releasing agent able to copolymerize with the comonomeric blend, improving the restorative material's properties.
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http://dx.doi.org/10.1590/0103-6440201701346 | DOI Listing |
Int J Mol Sci
January 2025
Laboratory of Bioorganic Compounds Synthesis and Analysis, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, Poland.
The biological and thermal properties of a class of synthetic dihydroimidazotriazinones were disclosed in this article for the first time. Molecules --as potential innovative antimetabolites mimicking bicyclic aza-analogues of isocytosine-were evaluated for their in vitro anticancer activity. Moreover, in vivo, in vitro, and ex vivo toxicity profiles of all the compounds were established in zebrafish, non-tumour cell, and erythrocyte models, respectively.
View Article and Find Full Text PDFChem Biodivers
January 2025
NMIMS Deemed to be University - Mumbai Campus: NMIMS, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SPPSPTM, VILE PARLE WEST, 400056, Mumbai, INDIA.
Acetohydroxyacid synthase (AHAS) is a vital enzyme in Mycobacterium tuberculosis, the pathogen causing tuberculosis (TB), involved in branched-chain amino acid synthesis. Targeting AHAS for drug design against TB offers a promising strategy due to its essentiality in bacterial growth. In current investigation, we have designed 160 novel compounds by leveraging key scaffolds identified through structure-based drug design (SBDD) methodologies.
View Article and Find Full Text PDFBiochem Biophys Res Commun
January 2025
Molecular Biophysics and Structural Biology (MBSB) Group, Department of Biochemistry, University of Johannesburg, Auckland Park Kingsway Campus, 2006, South Africa. Electronic address:
To address microbial infections and combat drug resistance, we designed, synthesized, and evaluated three novel s-triazine clubbed pharmacophores: 1-acetylpyrazoline (5a-e), 2-aminopyrimidine (6a-e), and 1,5-benzodiazepine (7a-e). These were derived from chalcone (4a-e), showing improved pharmacological profiles. The compounds underwent characterization by FTIR, NMR, and Mass Spectroscopy, and their antimicrobial activities, along with structure-activity relationships (SAR), were assessed using in silico and in vitro methods.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Ural Federal University named after the First President of Russia B.N. Eltsin, Mira st. 19, Yekaterinburg, 620002, Russian Federation.
A multi-component method for the synthesis of pyrimido[5,4-]azolo[1,5-]pyrimidines and pyrimido[4,5-][1,2,4]triazolo[5,1-][1,2,4]triazines has been developed. It was shown that vicinal amino-nitrile and amino-ethoxycarbonyl derivatives of azolo[1,5-]pyrimidines and azolo[5,1-][1,2,4]triazines were converted to tricyclic heterocycles in the "AcOH-RC(OEt)-amine" system. Reaction conditions were optimized, patterns of this process were investigated, and intermediates were isolated.
View Article and Find Full Text PDFFuture Med Chem
January 2025
Department of Chemistry, Faculty of Science, Ain Shams University, Cairo, Egypt.
Aim: New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized.
Methods & Results: Cytotoxicity of our derivatives was estimated on four cancer and VERO normal cell lines targeting EGFR (epidermal growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) enzymes. Our new derivatives selectively inhibited both VEGFR-2 and EGFR as they have the essential structural requirements for inhibitors of both receptors.
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