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Identification of novel azaindazole CCR1 antagonist clinical candidates.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Feb 01; Vol. 29 (3), pp. 441-448. Date of Electronic Publication: 2018 Dec 13. - Publication Year :
- 2019
-
Abstract
- Exploring various cyclization strategies, using a submicromolar pyrazole HTS screening hit 6 as a starting point, a novel indazole based CCR1 antagonist core was discovered. This report presents the design and SAR of CCR1 indazole and azaindazole antagonists leading to the identification of three development compounds, including 19e that was advanced to early clinical trials.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Aza Compounds chemical synthesis
Aza Compounds chemistry
Dose-Response Relationship, Drug
Drug Design
Humans
Indazoles chemical synthesis
Indazoles chemistry
Molecular Structure
Receptors, CCR1 metabolism
Structure-Activity Relationship
Aza Compounds pharmacology
Indazoles pharmacology
Receptors, CCR1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30595446
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.12.024