In conjunction with CXCR4, the G protein coupled receptor CXCR7 has been reported to play a protective role following a cardiac event to improve both function and cardiac injury repair processes. It was postulated that a potent small molecule CXCR7 modulator could interact with the target receptor to prevent binding, internalization, and degradation of its natural ligand SDF1α. Following a rigorous medicinal chemistry campaign targeting upregulation of the systemic circulation of SDF1α, a sterically hindered tertiary beta amino amide was identified as a promising candidate. The work presented herein highlights the project rationale, key SAR developed en route to the discovery of our in vivo tool compound, and the practical asymmetric synthesis that bridged our initial discovery route to enable the delivery of bulk quantities to support critical in vivo studies.

Discovery and asymmetric synthesis of potent and selective small-molecule modulators of CXCR7 for treatment for cardiac fibrosis

Macromolecular Chemistry: The Second Century

[Author Benefits](https://scimeetings.acs.org/?utm_source=pubs_content_marketing&utm_medium=website&utm_campaign=0320_MCF_NPI_Launch_Spring_Homepage&ref=pubs_content_marketing)

[How to use SciMeetings](https://storage.googleapis.com/dl.morressier.com/acs/SciMeetings-ACSSpring2020-HowToGuide_M3020-Final.pdf)

[Frequently Asked Questions](https://storage.googleapis.com/dl.morressier.com/acs/SciMtng_ACSNMSp2020_FAQ_M3120_Final.pdf)

ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.