Using reversed-phase high-performance thin-layer chromatography and a methanol-water mixture as the mobile phase, the lipophilicity of 12 new synthesized derivatives is studied. The first eight compounds have as a basic chemical structure aryliden-hydrazino-selenazoles, and the second group of the three compounds belongs to aroyl-hydrazinoselenazoles. The linear correlation between R(Mw) and the methanol-water ratios showed high values for the correlation coefficient. The chromatographic hydrophobic index is determined by using the ratio -R(Mw)/S, and the obtained values ranged between 99 and 73. A good linear correlation is obtained between R(Mw) and the slope. The log P values are calculated using ACD/Labs Software. The matrices are formed with R(Mw) and log P and are subjected to a principal component analysis (PCA). The best way to extract information from PCA is graphically, by plotting the obtained matrices. By analyzing the scores, the compounds can be grouped as follows: a group containing nine compounds, and a second one containing three compounds. Each group of compounds has the same basic chemical structure.
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http://dx.doi.org/10.1093/chromsci/bmr034 | DOI Listing |
Bioorg Chem
January 2025
Department of Chemistry, St Berchmans College (Autonomous), Changanassery, Kerala 686101, India; Centre for Theoretical and Computational Chemistry, St Berchmans College (Autonomous), Changanassery, Kerala 686101, India. Electronic address:
In this study, three novel derivatives of benzo[b]thiophene-2-carbaldehyde (BTAP1, BTAP2, and BTAP3) were successfully synthesized and comprehensively characterized using spectroscopic techniques including FTIR, UV-VIS, HNMR, and CNMR. Thermal analysis through TGA and DTA demonstrated remarkable thermal stability with a maximum threshold at 270 °C. Spectroscopic investigations revealed π → π* transitions in all compounds, attributed to the conjugated system comprising benzothiophene rings connected to bromophenyl/ aminophenyl/phenol rings via α, β-unsaturated ketone bridges.
View Article and Find Full Text PDFACS Chem Neurosci
January 2025
Sensor Engineering Department, Faculty of Science and Engineering, Maastricht University, 6200 MD Maastricht, The Netherlands.
As the main inhibitory neurotransmission system, the GABAergic system poses an interesting yet underutilized target for molecular brain imaging. While PET imaging of postsynaptic GABAergic neurons has been accomplished using radiolabeled benzodiazepines targeting the GABA receptor, the development of presynaptic radioligands targeting GABA transporter 1 (GAT1) has been unsuccessful thus far. Therefore, we developed a novel GAT1-addressing radioligand and investigated its applicability as a PET tracer in rodents.
View Article and Find Full Text PDFChem Biodivers
January 2025
Ordu University: Ordu Universitesi, Department of Chemistry, Cumhuriyet Mah., Ordu, TURKEY.
The concise synthesis of O-methyled-inositol derivative and conduritol derivatives was obtained starting from p-benzoquinone. Spectroscopic methods have been performed for characterization of new synthesized compounds. Cyclitols are useful molecules with anticancer, antibiotic, antinutrient and antileukemic activity.
View Article and Find Full Text PDFCurr Top Dev Biol
January 2025
Department of Pharmaceutics, School of Pharmacy, University of Washington.
The active metabolite of vitamin A, all-trans-retinoic acid (atRA), is critical for maintenance of many cellular processes. Although the enzymes that can synthesize and clear atRA in mammals have been identified, their tissue and cell-type specific roles are still not fully established. Based on the plasma protein binding, tissue distribution and lipophilicity of atRA, atRA partitions extensively to lipid membranes and other neutral lipids in cells.
View Article and Find Full Text PDFCarbohydr Res
January 2025
Department of Biomolecular Sciences, University of Urbino "Carlo Bo", Campus Scientifico E. Mattei, via Ca' Le Suore 2, 61029, Urbino, PU, Italy. Electronic address:
Cinnamic Acid Sugar Ester Derivatives (CASEDs) are a class of natural compounds that exhibit several interesting biological activities. However, to date, no examples of their use in sunscreen formulations have been reported. Here, we describe the synthesis of a series of novel cinnamic acid esters of glucose (4a-g), ribose (4h) and lactose (4i) starting from the respective acetals 3.
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