Bioorganic and Medicinal Chemistry Letters p. 511 - 516 (2007)
Update date:2022-08-04
Topics:
Asberom, Theodros
Zhao, Zhiqiang
Bara, Thomas A.
Clader, John W.
Greenlee, William J.
Hyde, Lynn A.
Josien, Hubert B.
Li, Wei
McPhail, Andrew T.
Nomeir, Amin A.
Parker, Eric M.
Rajagopalan, Murali
Song, Lixin
Wong, Gwendolyn T.
Zhang, Lili
Zhang, Qi
Pissarnitski, Dmitri A.
Attachment of the cyclopropylcarbamate group to the piperidine core of γ-secretase inhibitors leads to a dramatic increase of their in vitro potency. Strategies for subsequent improvement of the in vivo pharmacokinetic profile of the series are discussed.
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