Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors

DOI: 10.1016/j.bmcl.2007.08.013

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 5330 - 5335 (2007)

Update date:2022-08-11

Topics:

Authors:

Josien, Hubert

Bara, Thomas

Rajagopalan, Murali

Asberom, Theodros

Clader, John W.

Favreau, Leonard

Greenlee, William J.

Hyde, Lynn A.

Nomeir, Amin A.

Parker, Eric M.

Pissarnitski, Dmitri A.

Song, Lixin

Wong, Gwendolyn T.

Zhang, Lili

Zhang, Qi

Zhao, Zhiqiang

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Article abstract of DOI:10.1016/j.bmcl.2007.08.013

The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide γ-secretase inhibitors is reported. Lowering molecular weight including the use of conformational constraint led to compounds with less CYP 3A4 liability com

Full text of DOI:10.1016/j.bmcl.2007.08.013

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