Azaphenothiazine Conjugates: A New Class of Antimicrobial Compounds.

Although phenothiazines have been widely explored in medicinal chemistry for over a century, little attention has been paid to their pyridine analogs, azaphenothiazines. This article reports the first synthesis, characterization, and antimicrobial evaluation of S-oxide analogs of N-aminoalkylated azaphenothiazines as antibacterials and antifungals. The optimized synthetic protocol enabled the production of the desired azaphenothiazine sulfoxides 12a-e and sulfonyls 14a-e, respectively.

The Therapeutic Potential of Spirooxindoles in Cancer: A Focus on p53-MDM2 Modulation.

The p53, often referred to as the "guardian of the genome", is a well-established tumor-suppressor protein that plays a critical role in regulating the cell cycle, DNA repair, differentiation, and apoptosis, with its activity primarily modulated by the MDM2 protein (murine double minute 2, also known as HDM2 in humans). Disrupting the protein-protein interaction between p53 and MDM2 represents a promising therapeutic strategy for developing anticancer agents. Recent studies have shown that several spirooxindole-containing compounds exhibit significant antitumor properties, primarily by inhibiting the p53-MDM2 interaction.