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October 28, 2013Journal of Medicinal ChemistryOpen Access

Conformationally Constrained ortho-Anilino Diaryl Ureas: Discovery of 1-(2-(1′-Neopentylspiroindoline-3,4′-piperidine-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a Potent, Selective, and Bioavailable P2Y1 Antagonist

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Key result

Compound 3l, a novel P2Y1 antagonist, demonstrated a robust oral antithrombotic effect with mild bleeding liability in rat thrombosis and hemostasis models.

Why the study?

Does the novel P2Y1 antagonist compound 3l provide oral antithrombotic efficacy with reduced bleeding liability in rat models?

Population

Preclinical rat models for thrombosis and hemostasis

Design

Preclinical

Authors

JQJennifer X. QiaoTWTammy C. WangRRRéjean Ruel

Discussion

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Overview

Supports progression to human studies for oral antithrombotic therapy; leaves open efficacy and safety in patients.

Structured PICO

Does the novel P2Y1 antagonist compound 3l provide oral antithrombotic efficacy with reduced bleeding liability in rat models?

P
Population
Preclinical rat models for thrombosis and hemostasis
I
Intervention
Compound 3l (a conformationally constrained ortho-anilino diaryl urea P2Y1 antagonist)
O
Outcome
Oral antithrombotic effect and bleeding liabilitysurrogate

Compound 3l is a novel, orally bioavailable P2Y1 antagonist that shows robust antithrombotic efficacy with mild bleeding liability in preclinical rat models.

Cite This Study

Qiao et al. (2013) studied Thrombosis. Compound 3l (P2Y1 antagonist) was evaluated on Antithrombotic effect and bleeding liability in rat models. Compound 3l, a novel P2Y1 antagonist, demonstrated a robust oral antithrombotic effect with mild bleeding liability in rat thrombosis and hemostasis models.

synapsesocial.com/papers/6a5ccca57d25ef04d2c4fb60https://doi.org/10.1021/jm4013906
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