90000-67-2Relevant articles and documents
KETONE INHIBITORS OF LYSINE GINGIPAIN
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Paragraph 0434, (2018/04/12)
The present invention provides compounds according to Formula (I) as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-Heteroarylthiomethyldipyridodiazepinone derivatives
Yoakim,Bonneau,Deziel,Doyon,Duan,Guse,Landry,Malenfant,Naud,Ogilvie,O'Meara,Plante,Simoneau,Thavonekham,Boes,Cordingley
, p. 739 - 742 (2007/10/03)
A series of 8-heteroarylthiomethyldipyridodiazepinone derivatives were prepared and evaluated for their antiviral profile against wild type virus and the important K103N/Y181C mutant as an indicator for broad activity. 2,6-Dimethylpyridine derivative 16 was found to have a good pharmacokinetic profile in spite of poor metabolic stability in rat liver microsomes.