The objective of this work was to design conjugates of anti-HIV nucleosides conjugated with fatty acids and cell-penetrating poly-L-arginine (polyArg) peptides. Three conjugates of polyArg cell-penetrating peptides with fatty acyl derivatives of alovudine (FLT), lamivudine (3TC), and emtricitabine (FTC) were synthesized. In general, the compounds exhibited anti-HIV activity against X4 and R5 cell-free virus with EC50 values of 1.5-16.6 μM. FLT-CO-(CH2)12-CO-(Arg)7 exhibited EC50 values of 2.9 μM and 3.1 μM against X4 and R5 cell-free virus, respectively. The FLT conjugate was selected for further preformulation studies by determination of solution state degradation and lipid solubility. The compound was found to be stable in neutral and oxidative conditions and moderately stable in heated conditions.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4269296 | PMC |
http://dx.doi.org/10.1080/15257770.2014.945649 | DOI Listing |
Arch Biochem Biophys
January 2025
Department of Biosciences Grand Asian University of Sialkot, Pakistan.
Acyl thiourea scaffolds are frequently employed in drug development to discern unique and essential therapies for the eradication of the most challenging diseases. Hence, we developed a library of novel cyclopropyl incorporating acyl thiourea derivatives (4a-j) and evaluated their antimicrobial, α-amylase, and proteinase K inhibition potential. Compound (4h) (4-methoxy) demonstrated the strongest α-amylase inhibition (IC = 1.
View Article and Find Full Text PDFBiochem Biophys Res Commun
January 2025
Depto. de Química Biológica Ranwel Caputto. Facultad. Ciencias Químicas. Univ. Nacional de Córdoba, Argentina; Centro de Investigaciones en Química Biológica de Córdoba (CIQUIBIC) CONICET, Córdoba, Argentina. Electronic address:
Lipophilic derivatives of vitamin C, known as ascorbyl-6-O-alkanoates (ASCn), have been mainly developed for use in cosmetics, pharmaceuticals, and the food industry as antioxidant additives. These derivatives are of biotechnological interest due to their antioxidant properties, amphiphilic behavior, capacity to self-organize into nano- and micro-structures, anionic nature, and low cost of synthesis. In this review, we will focus on the commercial amphiphile, 6-O-palmitoyl L-ascorbic acid (ASC16), and the shorter acyl chains derivatives, such as 6-O-myristoyl (ASC14) and 6-O-lauroyl L-ascorbic acid (ASC12).
View Article and Find Full Text PDFChem Asian J
January 2025
Indian Institute of Science Education and Research Thiruvananthapuram, chemistry, 2204, School of Chemistry, Vithura, 695551, Thiruvananthapuram, INDIA.
A one-pot methodology for the tandem acylation and oxidative aromatization of vinylogous thioesters to 2-acyl-5-(alkyl/arylthio)phenols is presented. Initially, cyclohexane-1,3-diones were converted to vinylogous thioesters through FeCl3-mediated thioenolization. This was followed by LiTMP-mediated acylation and DDQ-mediated aromatization, which resulted in the synthesis of sulphur derived oxybenzone analogs.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Agricultural, Food and Nutritional Science, University of Alberta, Edmonton, AB, T6G2P5, Canada.
J Phys Chem B
January 2025
INSERM U1248 Pharmacology & Transplantation, Univ. Limoges, CBRS, 2 Rue du Prof. Descottes, F-87000 Limoges, France.
Dry skin is a common condition that is experienced by many. Besides being particularly present during the cold season, various diseases exist all year round, leading to localized xerosis. To prevent it, the skin is provided with natural moisturizing factors (NMFs).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!