Abstract
Vorapaxar is an approved drug for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Subsequent to the discovery of Vorapaxar, medicinal chemistry efforts were continued to identify structurally differentiated leads. Toward this goal, extensive structure-activity relationship studies using a C-ring-truncated version of Vorapaxar culminated in the discovery of three leads, represented as 13, 14, and 23. Among these leads, compound 14 possessed favorable pharmacokinetic properties and an off-target profile, which supported additional profiling in an exploratory rat toxicology study.
Original language | English (US) |
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Pages (from-to) | 5575-5592 |
Number of pages | 18 |
Journal | Journal of medicinal chemistry |
Volume | 65 |
Issue number | 7 |
DOIs | |
State | Published - Apr 14 2022 |
ASJC Scopus subject areas
- Drug Discovery
- Molecular Medicine