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netLibrary - eBook Summary Structure-based Drug Design by ...

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Document<br />

Page 256<br />

The discovery program proceeded in four iterative phases which are shown in Table 1. Initial screening<br />

of low molecular weight organic bases led to the discovery of 1-amidinopiperidine (1–1) as a new<br />

surrogate for the guanidine and amidine functionality in Argatroban and NAPAP, respectively. A<br />

distinct advantage of 1-amidinopiperidine is its intrinsic selectivity for thrombin over<br />

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