1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.

Arbuckle, Wullie; Baugh, Mark; Belshaw, Simone; Bennett, D Jonathan; Bruin, John; Cai, Jiaqiang; Cameron, Kenneth S; Claxton, Chris; Dempster, Maureen; Everett, Kathryn; Fradera, Xavier; Hamilton, William; Jones, Philip S; Kinghorn, Emma; Long, Clive; Martin, Iain; Robinson, John; Westwood, Paul

Arbuckle, Wullie; Baugh, Mark; Belshaw, Simone; Bennett, D Jonathan; Bruin, John; Cai, Jiaqiang; Cameron, Kenneth S; Claxton, Chris; Dempster, Maureen; Everett, Kathryn; Fradera, Xavier; Hamilton, William; Jones, Philip S; Kinghorn, Emma; Long, Clive; Martin, Iain; Robinson, John; Westwood, Paul.

Affiliation

Arbuckle W; Merck Research laboratories, MSD, Lanarkshire ML1 5SH, United Kingdom.

Bioorg Med Chem Lett ; 21(3): 932-5, 2011 Feb 01.

Article in En | MEDLINE | ID: mdl-21227690

Subject(s)

Cathepsins/antagonists & inhibitors; Nitrogen/chemistry; Protease Inhibitors/chemistry; Pyridines/chemistry; Animals; Cathepsins/metabolism; Mice; Protease Inhibitors/chemical synthesis; Protease Inhibitors/pharmacokinetics; Pyridines/chemical synthesis; Pyridines/pharmacokinetics; Rats; Rats, Sprague-Dawley

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protease Inhibitors / Pyridines / Cathepsins / Nitrogen Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Type: Article Affiliation country: United kingdom

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