425397-69-9Relevant academic research and scientific papers
4-Fluorobenzylpiperazine-Containing Derivatives as Efficient Inhibitors of Mushroom Tyrosinase
De Luca, Laura,Fais, Antonella,Floris, Sonia,Germanò, Maria Paola,Gitto, Rosaria,Ielo, Laura,Mirabile, Salvatore,Rapisarda, Antonio,Vittorio, Serena
, p. 1757 - 1764 (2020)
Tyrosinase is a type-3 copper protein involved in the biosynthesis of melanin pigments; therefore, the inhibition of its enzymatic activity represents a promising strategy for the treatment of hyperpigmentation-related disorders. To address this point, we previously designed a class of 4-(4-fluorobenzyl)piperazin-1-yl-based compounds, which proved to be more active inhibitors against tyrosinase from mushroom Agaricus bisporus than the positive control kojic acid. Herein, we report the synthesis of further series of 4-(4-fluorobenzyl)piperazin-1-yl analogues bearing a (hetero)aromatic fragment as key feature to improve protein affinity. The newly synthesized compounds were assayed in vitro and proved to be potent inhibitors in the low-micromolar range. The active 2-thienyl and 2-furyl derivatives were selected for further modification to allow their binding mode to be analyzed by docking studies and to give satisfactory safety profiles.
Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase
Laufer, Stefan,Lehmann, Frank
supporting information; experimental part, p. 1461 - 1464 (2009/11/30)
The p38 MAP kinase is implicated in the release of the pro-inflammatory cytokines TNFα and IL-1b. Inhibition of cytokine release may be a useful treatment for inflammatory conditions such as rheumatoid arthritis and Crohn's disease. A new lead structure for p38 MAP kinase inhibition was identified. Herein, we report the SAR of this new class of p38 inhibitors.
