861856-61-3Relevant articles and documents
Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in staphylococcus aureus
Song, Yongcheng,Lin, Fu-Yang,Yin, Fenglin,Hensler, Mary,Poveda, Carlos A. Rodrígues,Mukkamala, Dushyant,Cao, Rong,Wang, Hong,Morita, Craig T.,Pacanowska, Dolores González,Nizet, Victor,Oldfield, Eric
experimental part, p. 976 - 988 (2009/12/04)
Staphylococcus aureus produces a golden carotenoid virulence factor called staphyloxanthin (STX), and we report here the inhibition of the enzyme, dehydrosqualene synthase (CrtM), responsible for the first committed step in STX biosynthesis. The most acti
Structure-activity relationships of α-ketooxazole inhibitors of fatty acid amide hydrolase
Hardouin, Christophe,Kelso, Michael J.,Romero, F. Anthony,Rayl, Thomas J.,Leung, Donmienne,Hwang, Inkyu,Cravatt, Benjamin F.,Boger, Dale L.
, p. 3359 - 3368 (2008/02/13)
A systematic study of the structure-activity relationships of 2b (OL-135), a potent inhibitor of fatty acid amide hydrolase (FAAH), is detailed targeting the C2 acyl side chain. A series of aryl replacements or substituents for the terminal phenyl group provided effective inhibitors (e.g., 5c, aryl = 1-napthyl, K, - 2.6 nM), with 5hh (aryl -3-ClPh, Ki = 900 pM) being 5-fold more potent than 2b. Conformationally restricted C2 side chains were examined, and many provided exceptionally potent inhibitors, of which 11j (ethylbiphenyl side chain) was established to be a 750 pM inhibitor. A systematic series of heteroatoms (O, NMe, S), electron-withdrawing groups (SO, SO2), and amides positioned within and hydroxyl substitutions on the linking side chain were investigated, which typically led to a loss in potency. The most tolerant positions provided effective inhibitors (12p, 6-position S, Ki = 3 nM, or 13d, 2-position OH, Ki = 8 nM) comparable in potency to 2b. Proteome-wide screening of selected inhibitors from the systematic series of >100 candidates prepared revealed that they are selective for FAAH over all other mammalian serine proteases.
GUANIDINOTHIAZOLYL DERIVATIVES
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, (2008/06/13)
The compounds are guanidinothiazolyl derivatives which are histamine H. sub.2-antagonists. A specific compound of the present invention is 2-2-(2-guanidino-4-thiazolylmethylthio)ethylamino!-5-(6-methyl-3-pyridylmethy l)-4-pyrimidone.