November 12, 1998Journal of Medicinal ChemistryOpen Access

Tetrahydro-isoquinoline-Based Factor Xa Inhibitors

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Population

In vitro biochemical assays and molecular modeling of factor Xa (fXa)

Design

Preclinical

Authors

RKRalf KucznierzRoche (United States)FGFrank GramsRoche (Switzerland)HLHerbert LeinertDarmstadt University of Applied Sciences

Discussion

Member takes

Implication

Merits preclinical testing as anticoagulants; leaves open clinical translation.

Structured PICO

Population

In vitro biochemical assays and molecular modeling of factor Xa (fXa)

Intervention

Derivatives of (2-amidino-1,2,3, 4-tetrahydro-isoquinolin-7-yloxy)phenylacetic acid (TIPAC)

Outcome

Inhibition constants (Ki) for factor Xa, thrombin, and trypsinsurrogate

Novel tetrahydro-isoquinoline-based compounds demonstrate potent and selective inhibition of factor Xa in vitro, with molecular modeling suggesting a specific two-site binding mode.

Cite This Study

Kucznierz et al. (1998) studied this question.

synapsesocial.com/papers/6a898c81451a22fc7efb8f08 https://doi.org/10.1021/jm9800402

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