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A series of acyclic selenopurine nucleosides 3a–f and 4a–g were synthesized based on the bioisosteric rationale between oxygen and selenium, and then evaluated for antiviral activity. Among the compounds tested, seleno-acyclovir (4a) exhibited the most potent anti-herpes simplex virus (HSV)-1 (EC50 = 1.47 µM) and HSV-2 (EC50 = 6.34 µM) activities without cytotoxicity up to 100 µM, while 2,6-diaminopurine derivatives 4e–g exhibited significant anti-human cytomegalovirus (HCMV) activity, which is slightly more potent than the guanine derivative 4d, indicating that they might act as prodrugs of seleno-ganciclovir (4d).

Salicylate-based poly(anhydride-esters; SAPAEs) have demonstrated wound healing properties due to salicylic acid (SA) release during polymer degradation. Additionally, the polymers are deformable and self-adhesive due to their low Young's modulus, lower glass transition temperature (T g), and inherent tackiness at body temperature. These properties make them particularly well-suited for therapeutic use in the bacteria-laden environment of the oral cavity. To enhance their therapeutic capabilities, the antiseptic chlorhexidine dihydrochloride was physically incorporated into SAPAEs for dual release of antiseptic and anti-inflammatory upon degradation. This study analyzes the thermomechanical properties of two SAPAE compositions (adipate homopolymer and 50:50 adipate:sebacate copolymer) and the release of chlorhexidine (incorporated at 10% (w/w)) from these polymers. Polymer adhesivity was monitored as a function of chlorhexidine incorporation and in vitro degradation time. Throughout in vitro degradation, the polymer systems had a low Young's modulus and a T g at or near body temperature. Incorporation of the antiseptic further decreased Young's modulus and increased both the T g and adhesivity. The release profiles were also evaluated and determined to be similar for the homopolymer and copolymer, although the homopolymer degradation occurred over a longer time period. Overall, the SAPAE systems have favorable properties for periodontal disease treatments by virtue of their controlled degradability, deformability, adhesivity, and release profiles with encapsulated antiseptic. [ABSTRACT FROM AUTHOR]

Fluorescence monitoring of ATP in different organelles is now feasible with a few biosensors developed, which, however, show low sensitivity, limited biocompatibility, and accessibility. Small‐molecule ATP probes that alleviate those limitations thus have received much attention recently, leading to a few ATP probes that target several organelles except for the nucleus. We disclose the first small‐molecule probe that selectively detects nuclear ATP through reversible binding, with 25‐fold fluorescence enhancement at pH 7.4 and excellent selectivity against various biologically relevant species. Using the probe, we observed 2.1–3.3‐fold and 3.9–7.8‐fold higher nuclear ATP levels in cancerous cell lines and tumor tissues compared with normal cell lines and tissues, respectively, which are explained by the higher nuclear ATP level in the mitosis phase. The probe has great potential for studying nuclear ATP‐associated biology. [ABSTRACT FROM AUTHOR]

Onthe basis of the potent antiviral activity of acyclovir andganciclovir, selenoacyclovir (2a) and selenoganciclovir(2b) were designed based on bioisoteric rationale andsynthesized via the diselenide 7as the key intermediate.Compound 2aexhibited potent anti-HSV-1 and -2 activitieswhile 2bexerted moderate anti-HCMV activity, indicatingthat these nucleosides can serve as a novel template for the developmentof new antiviral agents. [ABSTRACT FROM AUTHOR]