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Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

Authors :
Mattson MN
Neitzel ML
Quincy DA
Semko CM
Garofalo AW
Keim PS
Konradi AW
Pleiss MA
Sham HL
Brigham EF
Goldbach EG
Zhang H
Sauer JM
Basi GS
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Apr 01; Vol. 20 (7), pp. 2148-50. Date of Electronic Publication: 2010 Feb 14.
Publication Year :
2010

Abstract

Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance.<br /> (2010 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
20
Issue :
7
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
20206516
Full Text :
https://doi.org/10.1016/j.bmcl.2010.02.050