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Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).

Abstract：

:Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochemical properties are highlighted and the pharmacokinetic profiles of representative compounds is presented.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Behnke D,Cotesta S,Hintermann S,Fendt M,Gee CE,Jacobson LH,Laue G,Meyer A,Wagner T,Badiger S,Chaudhari V,Chebrolu M,Pandit C,Hoyer D,Betschart C

doi

10.1016/j.bmcl.2015.10.055

subject

Has Abstract

pub_date

2015-12-01 00:00:00

pages

5555-60

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)30164-5

journal_volume

25

pub_type

杂志文章

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