In 2015,Parsy, Christophe C.; Alexandre, Francois-Rene; Bidau, Valerie; Bonnaterre, Florence; Brandt, Guillaume; Caillet, Catherine; Cappelle, Sylvie; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa B.; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Chiara, Musiu; Roques, Virginie; Rosinovsky, Elodie; Savin, Simon; Seifer, Maria; Standring, David; Surleraux, Dominique published 《Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320》.Bioorganic & Medicinal Chemistry Letters published the findings.Electric Literature of C4H3F3N2 The information in the text is summarized as follows:
Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity. This research led to the selection of clin. candidate IDX320 having good genotype coverage and pharmacokinetic properties in various species. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature of C4H3F3N2)
3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Electric Literature of C4H3F3N2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics