856843-02-2Relevant academic research and scientific papers
Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)
Bonfanti, Jean-Fran?ois,Meyer, Christophe,Doublet, Frédéric,Fortin, Jér?me,Müller, Philippe,Queguiner, Laurence,Gevers, Tom,Janssens, Peggy,Szel, Heidi,Willebrords, Rudy,Timmerman, Philip,Wuyts, Koen,Van Remoortere, Pieter,Janssens, Frans,Wigerinck, Piet,Andries, Koen
, p. 875 - 896 (2008/09/19)
A preceding paper (Bonfanti et al. J. Med Chem. 2007, 50, 4572-4584) reported the optimization of the pharmacokinetic profile of substituted benzimidazoles by reducing their tissue retention. However, the modifications that were necessary to achieve this goal also led to a significant drop in anti-RSV activity. This paper describes a molecular modeling study followed by a lead optimization program that led to the recovery of the initial potent antiviral activity and the selection of TMC353121 as a clinical candidate.
AMINOBENZIMIDAZOLES AND BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
-
Page/Page column 40, (2008/06/13)
Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula (I) the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct b
