Key result
7-fluoroindazoles demonstrated about 60-fold greater factor Xa inhibitory potency compared to corresponding indazoles without the 7-fluoro group.
Population
Factor Xa enzyme (in vitro and cocrystal structures)
Comparison
7-fluoroindazoles vs Corresponding indazoles lacking the 7-fluoro group
Design
Preclinical
Authors
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Guides factor Xa inhibitor optimization; leaves open clinical translation from this animal model.
Effect estimate: 60-fold greater
A novel 7-fluoroindazolyl moiety significantly increases the potency of factor Xa inhibitors by forming a key hydrogen bond with the enzyme's beta-sheet domain.
Lee et al. (2007) studied Factor Xa inhibition. 7-fluoroindazoles vs. corresponding indazoles was evaluated on Factor Xa inhibitory potency (60-fold greater). 7-fluoroindazoles demonstrated about 60-fold greater factor Xa inhibitory potency compared to corresponding indazoles without the 7-fluoro group.
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