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

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.

Jansson, Juliette (author)
Ray, Colin (author)
Rosqvist, Susanne (author)
Gustavsson, Susanne (author)
Nilsson, Linda I (author)
Minidis, Alexander (author)
Holenz, Jörg (author)
Rotticci, Didier (author)
Lundkvist, Johan (author)
Arvidsson, Per I.Uppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)pearv049 (author)
Uppsala universitetAvdelningen för organisk farmaceutisk kemi (creator_code:org_t)

By the author/editor: Sehgelmeble, Fer ...; Jansson, Juliett ...; Ray, Colin; Rosqvist, Susann ...; Gustavsson, Susa ...; Nilsson, Linda I; show more...; Minidis, Alexand ...; Holenz, Jörg; Rotticci, Didier; Lundkvist, Johan; Arvidsson, Per I ...; show less...

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Medicinal Chemis ...

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