854133-07-6Relevant articles and documents
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones
Shcherbakova, Irina,Huang, Guangfei,Geoffroy, Otto J.,Nair, Satheesh K.,Swierczek, Krzysztof,Balandrin, Manuel F.,Fox, John,Heaton, William L.,Conklin, Rebecca L.
, p. 2537 - 2540 (2005)
Design, new synthesis, structure-activity relationship studies and calcium receptor antagonist (calcilytic) properties of novel 3H-pyrimidin-4-ones are described.
MODULATORS FOR AMYLOID BETA
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Page/Page column 43, (2009/07/25)
The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
Multicomponent reactions involving tricyclooxonium ylide intermediate: Diastereoselective synthesis of mono- and bisalkoxyoctahydro-1,4-benzodioxocin- 6(5H)-one frameworks
Muthusamy, Sengodagounder,Krishnamurthi, Janagiraman,Suresh, Eringathodi
, p. 861 - 863 (2007/10/03)
A highly diastereoselective tandem ring-enlargement and aldol condensation process involving multicomponent reactions of ethereal tricyclooxonium ylide intermediate with alcohols, mono- or dialdehydes in the presence of titanium(iv) isopropoxide is descri
CALCILYTIC COMPOUNDS
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Page/Page column 150-151, (2008/06/13)
Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
Design of inhibitors of scytalone dehydratase: Probing interactions with an asparagine carboxamide
Basarab, Gregory S.,Jordan, Douglas B.,Gehret, Troy C.,Schwartz, Rand S.
, p. 4143 - 4154 (2007/10/03)
Among the active-site residues of scytalone dehydratase, the side-chain carboxamide of asparagine 131 has the greatest potential for strong electrostatic interactions. Structure-based inhibitor design aimed at enhancing interactions with this residue led to the synthesis of a series of highly potent inhibitors that have a five- or six-membered ring containing a carbonyl functionality for hydrogen bonding. To achieve a good orientation for hydrogen bonding, the inhibitors incorporate a phenyl substituent that displaces a phenylalanine residue away from the five- or six-membered rings. Without the phenyl substituent, inhibitor binding potency is diminished by three orders of magnitude. Larger Ki values of a site-directed mutant (Asn131Ala) of scytalone dehydratase in comparison to those of wild-type enzyme validate the design concept. The most potent inhibitor (Ki=15 pM) contains a tetrahydrothiophenone that can form a single hydrogen bond with the asparagine carboxamide. Inhibitors with a butyrolactam that can form two hydrogen bonds with the asparagine carboxamide demonstrate excellent in vivo fungicidal activity.
An efficient large scale synthesis of 2-methoxytetrahydrophenanthridine
Hay,Denny
, p. 463 - 470 (2007/10/03)
A practical and high yielding synthesis of 2-methoxy-7,8,9,10-tetrahydrophenanthridine suitable for large-scale preparation is described.