Article
Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121).
Journal of medicinal chemistry - 28 Feb 2008
Bonfanti Jean-François, Meyer Christophe, Doublet Frédéric, Fortin Jérôme, Muller Philippe, Queguiner Laurence, Gevers Tom, Janssens Peggy, Szel Heidi, Willebrords Rudy, Timmerman Philip, Wuyts Koen, van Remoortere Pieter, Janssens Frans, Wigerinck Piet, Andries Koen
Abstract excerpt
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...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.