Journal article
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
Bioorganic & medicinal chemistry letters, v 18(14), pp 3852-3855
15 Jul 2008
PMID: 18595693
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
A series of aniline-substituted tetrahydroquinoline C5aR antagonists with distinct structure-activity relationships are presented.
A series of aniline-substituted tetrahydroquinoline C5a receptor antagonists were discovered. A functionality requirement of
ortho substitution on the aniline was revealed. Secondary anilines, in general, outperformed tertiary analogs in inhibition of C5a-induced calcium mobilization. Further enhancement of activity was realized in the presence of an
ortho hydroxyalkyl side chain. The functional IC
50 of selected analogs was optimized to the single-digit nanomolar level.
Metrics
Details
- Title
- Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
- Creators
- Yong Gong - Johnson & Johnson (United States)J. Kent Barbay - Johnson & Johnson (United States)Mieke Buntinx - Johnson & Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, B-2340 Beerse, BelgiumJian Li - Johnson & Johnson (United States)Jean Van Wauwe - Johnson & Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, B-2340 Beerse, BelgiumConcha Claes - Johnson & Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, B-2340 Beerse, BelgiumGuy Van Lommen - Johnson & Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, B-2340 Beerse, BelgiumPamela J. Hornby - Johnson & Johnson (United States)Wei He - Johnson & Johnson (United States)
- Publication Details
- Bioorganic & medicinal chemistry letters, v 18(14), pp 3852-3855
- Publisher
- Elsevier
- Number of pages
- 4
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000257640400003
- Scopus ID
- 2-s2.0-47149108682
- Other Identifier
- 991021931779504721
UN Sustainable Development Goals (SDGs)
This publication has contributed to the advancement of the following goals:
InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Collaboration types
- International collaboration
- Web of Science research areas
- Chemistry, Medicinal
- Chemistry, Organic