nitrophenols and thiosemicarbazide

Intracellular viscosity is a physicochemical factor that determines the outcomes of various biological processes, while nitric oxide (NO) is an essential signaling molecule that controls many cellular processes, including oxidative stress. Anticipating that both may be interrelated with a variety of pathologies, their simultaneous measurement would be highly valuable for the investigation of the pathological condition of cells. However, the development of a sensor for such simultaneous detection has not been attempted yet. Herein, we present the synthesis of naphthalimide-4-(4-nitrophenyl)thiosemicarbazide, probe

Topics: Fluorescent Dyes; HeLa Cells; Humans; Microscopy, Fluorescence; Naphthalimides; Nitric Oxide; Nitrophenols; Semicarbazides; Viscosity

A series of thiosemicarbazides with 4-nitrophenyl group was obtained in the reaction of carboxylic acid hydrazides with isothiocyanates. All compounds were checked for their antibacterial and antiproliferative activity. Our results have shown that derivatives 6-8 possessed antibacterial activity against S. aureus, S. epidermidis, S. mutans and S. sanguinis, moderate cytotoxicity and good therapeutic safety in vitro. Additionally, compounds 1 and 4 significantly inhibited A549, HepG2 and MCF-7 cell division. Moreover, PASS software indicated that newly obtained compounds are potential α-glucosidase inhibitors. This was confirmed by in vitro studies. To investigate the mode of interaction with the molecular target compounds were docked to glucose binding site of the enzyme and exhibited a similar binding mode as glucose.

Topics: A549 Cells; Anti-Bacterial Agents; Bacteria; Binding Sites; Cell Line; Cell Proliferation; Glycoside Hydrolase Inhibitors; Hep G2 Cells; Humans; MCF-7 Cells; Molecular Docking Simulation; Nitrophenols; Semicarbazides; Structure-Activity Relationship