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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 26, 1996 - Issue 23
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Original Articles

Efficient Two-Step Syntheses of Sulfonylguanidines from Sulfonamides

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Pages 4299-4310 | Received 11 Mar 1996, Published online: 23 Aug 2006

References

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  • Sulfonylguanidines 5a-e, after saponification of the 5-ethyl ester on the imidazole ring, have been evaluated in vitro for their affinity for the AT1 receptor (ability to displace [125I]AII from its binding sites in rat liver membrane preparation)1. If they proved to be 5 to 10-fold less potent than the corresponding sulfonylurea HR 720, their in vitro potency was in similar range (2 - 5 nmol) to that of DuP 753, the only All antagonist on the market at the moment

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