Data for the synthesis of new 4-aryloxy-N-arylanilines as potent succinate-cytochrome c reductase inhibitors.

In this data article, we have designed a simple and facile protocol for copper-mediated synthesis of new 4-aryloxy-N-arylanilines under mild reaction conditions. The general information and synthetic procedures of all the target compounds were provided, and they were fully characterized by Nuclear Magnetic Resonance (NMR, including H NMR and C NMR), melting point measurements, and High-Resolution Mass Spectroscopy (HRMS). Furthermore, the inhibitory activities of these compounds against succinate-cytochrome c reductase (SCR) were evaluated, and the methods and procedures of enzyme inhibition experiments were also recorded in this data article.

Synthesis and photophysical properties of deuteration of pirfenidone.

In order to improve the metabolism of pirfenidone (5-methyl-1-phenylpyridin-2-one, PFD), the methyl-deuterated version of pirfenidone via the substitution of hydrogen (H) at C-5 by its isotope deuterium (D, 5D-PFD) was synthesized and its photophysical properties were investigated. The negative solvatochrom was observed in absorption and fluorescence spectra with increasing solvent polarity, which implied that intermolecular charge transfer (ICT) involved n → π* transition for both of PFD and 5D-PFD. The ground state and excited state dipole moment was calculated as 5.

Synthesis of new 4-aryloxy-N-arylanilines and their inhibitory activities against succinate-cytochrome c reductase.

Succinate-cytochrome c reductase (SCR) is composed of a mixture of mitochondrial complex II (succinate-ubiquinone oxidoreductase) and complex III (cytochrome bc complex). Meanwhile, complexes II and III are two promising targets of numerous antibiotics and fungicides. With an aim to identify new lead structures for SCR, complex II or III, a new series of 4-aryloxy-N-arylanilines were synthesized by introducing a 4-aryloxy phenyl group as one of the aryl groups in diaryl amines.