Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors.

19:00 EST 23rd November 2014 | BioPortfolio

Summary of "Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors."

The proof of the pudding: A proof-of-concept study using γ-secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for sulfonamides. Detailed in vitro and in vivo profiling reveal that the sulfonimidamide motif imparts desirable properties such as decreased lipophilicity and plasma protein binding, accompanied by increased solubility. Our data support a wider use of this unique functional group in the design of new pharmacologically active agents.

Affiliation

Medicinal Chemistry, iScience, CNSP iMed, AstraZeneca R&D Södertälje, Västra Mälarehamnen 9, 151 85 Södertälje (Sweden).

Journal Details

This article was published in the following journal.

Name: ChemMedChem
ISSN: 1860-7187
Pages: 396-9

Links

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