A5044017093- Biochemical and Molecular Research
- Mosquito-borne diseases and control
- Malaria Research and Control
- RNA and protein synthesis mechanisms
- HIV Research and Treatment
- HIV/AIDS drug development and treatment
- Viral Infections and Vectors
- Influenza Virus Research Studies
- Click Chemistry and Applications
Johnson & Johnson (United States)
2017
Janssen (Belgium)
2017
ABSTRACT Integration of viral DNA into the host chromosome is an essential step in life cycle retroviruses and facilitated by integrase enzyme. The first generation inhibitors recently approved or currently late-stage clinical trials shows great promise for treatment human immunodeficiency virus (HIV) infection, but expected to develop resistance these drugs. Therefore, we used a novel selection protocol follow emergence resistant HIV presence inhibitor elvitegravir (GS-9137). We find...
In the search for novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements 7-azaindole scaffold of Pimodivir, a PB2 (polymerase basic protein 2) inhibitor currently in clinical development. Specifically, 5,7-difluoroindole derivative 11a was identified potent and metabolically stable inhibitor. demonstrated favorable oral pharmacokinetic profile vivo efficacy mice. addition, it found that not at risk metabolism via aldehyde oxidase, an advantage over...