In silico screening and synthesis of stable tilmicosin-hydrazone derivatives as potential DNA disruptors towards Staphylococcus aureus.

In this study, 30 tilmicosin-hydrazone derivatives were designed using MOE software. Six candidate molecules with strong binding affinity to DNA or DNA-Topo II complexes, as indicated by molecular docking results, were synthesized. These candidates were evaluated for their in vitro antibacterial activities against common Gram-positive and Gram-negative bacteria.

Akt2 inhibition alleviates temporomandibular joint osteoarthritis by preventing subchondral bone loss.

Background: This study aimed to investigate the role and mechanism of the Akt2 pathway in different stages of anterior disc displacement (ADD)-induced temporomandibular joint osteoarthritis (TMJOA).

Methods: A rat model for TMJOA that simulates anterior disc displacement was established. For inhibit Akt2 expression in subchondral bone, rats were intravenously injected with adeno-associated virus carrying Akt2 shRNA at a titer of 1 × 10 transducing units/mL 10 days before the ADD or sham operations.