August 1, 1997Journal of Medicinal ChemistryOpen Access

Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

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Population

In vitro models for platelet GPIIb-IIIa receptor antagonism

Comparison

5,6-bicyclic amidines vs Freely flexible, acyclic benzamidine counterpart

Design

Preclinical

Authors

DSDaniel J. SallEli Lilly (United States)AAAnn ArfstenScripps Research Institute JBJolie BastianEli Lilly (United States)

Discussion

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Implication

Bicyclic amidines may boost GPIIb-IIIa antagonist potency in vitro; leaves open clinical translation and in vivo validation.

Structured PICO

Population

In vitro models for platelet GPIIb-IIIa receptor antagonism

Intervention

5,6-bicyclic amidines (conformationally restricted benzamidines)

Comparator

Freely flexible, acyclic benzamidine counterpart

Outcome

In vitro potency (GPIIb-IIIa receptor antagonism)surrogate

Conformationally restricted 5,6-bicyclic amidines act as potent arginine surrogates, significantly increasing the in vitro potency of platelet GPIIb-IIIa receptor antagonists.

Cite This Study

Sall et al. (1997) studied this question.

synapsesocial.com/papers/6a7cd019c6877338821d396e https://doi.org/10.1021/jm970020k

Topics

Dual antiplatelet therapy

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Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Topics

Also Consider