A closer look at N2,6-substituted 1,3,5-triazine-2,4-diamines: Advances in synthesis and biological activities.

N2,6-Substituted 1,3,5-triazine-2,4-diamines (N2-substituted guanamines) attracted significant interest due to their potential in the development of bioactive molecules. With just two points of diversity, this scaffold is proved to be suitable for constructing compounds targeting various enzymes, receptors, transporters, and nucleic acids with an array of therapeutic applications, particularly in cancer, inflammation, and CNS disorders. This review discusses progress in the synthesis of N2,6-substituted 1,3,5-triazine-2,4-diamines and their biological activities ranging from the inhibition of cancer-related enzymes (e.g. DNA topoisomerase IIα, carbonic anhydrases, ubiquitin-conjugating enzyme 2B, lysophosphatidic acid acyltransferase ß and various kinases) to the binding to CNS-relevant receptors (e.g. histamine H4, serotonin 5-HT6, adenosine A2a, and α7 nicotinic acetylcholine receptors).

Arabinoxylan-Carboxymethylcellulose Composite Films for Antibiotic Delivery to Infected Wounds.

Modern dressings should provide for local delivery of antibiotics and protect the wound from bacterial infection, dehydration and environmental factors to achieve optimal healing. The local delivery of antibiotics can reduce adverse effects and resistance challenges. In this study, we fabricated film dressings composed of arabinoxylan (AX) from Plantago ovata seed husks and carboxymethylcellulose (CMC) by a solvent cast method for the delivery of the antibiotic amikacin (AMK). To determine the suitability of the prepared AX-CMC composite films as wound dressings and drug delivery materials, their physical, chemical, mechanical, morphological, thermal, pharmaceutical, antimicrobial, cytocompatible, and drug delivery properties were investigated. The results demonstrated that the dressings were suitable for delivering the drug at the wound site in a sustained manner and keeping the environment moist for rapid healing. The AMK-loaded AX-CMC films exhibited controlled release of AMK, excellent antibacterial activity, and cytocompatibility. Thus, the AX-CMC composite films appear to be promising bioactive dressing materials for the prevention of wound infections.

Development and Characterization of Gentamicin-Loaded Arabinoxylan-Sodium Alginate Films as Antibacterial Wound Dressing.

Biopolymer-based antibacterial films are attractive materials for wound dressing application because they possess chemical, mechanical, exudate absorption, drug delivery, antibacterial, and biocompatible properties required to support wound healing. Herein, we fabricated and characterized films composed of arabinoxylan (AX) and sodium alginate (SA) loaded with gentamicin sulfate (GS) for application as a wound dressing. The FTIR, XRD, and thermal analyses show that AX, SA, and GS interacted through hydrogen bonding and were thermally stable. The AXSA film displays desirable wound dressing characteristics: transparency, uniform thickness, smooth surface morphology, tensile strength similar to human skin, mild water/exudate uptake capacity, water transmission rate suitable for wound dressing, and excellent cytocompatibility. In Franz diffusion release studies, >80% GS was released from AXSA films in two phases in 24 h following the Fickian diffusion mechanism. In disk diffusion assay, the AXSA films demonstrated excellent antibacterial effect against E.coli, S. aureus, and P. aeruginosa. Overall, the findings suggest that GS-loaded AXSA films hold potential for further development as antibacterial wound dressing material.