- Heteroaromatic moieties in the sphingosine backbone of α- Galactosylceramides for noncovalent interactions with CD1d
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A series of α-GalCer analogues containing heterocyclic and aromatic moieties in the sphingosine backbone were synthesized to improve the selectivity in the Th1/Th2 cytokine profile via noncovalent interaction with three aromatic residues at the binding pocket of CD1d. In vitro and in vivo biological evaluations revealed the treatment of α-GalCer analogue (6) induced the selective stimulation of natural killer T cells to facilitate the secretion of Th2 cytokines.
- Kim, Yongju,Kim, Jonghoon,Oh, Keunhee,Lee, Dong-Sup,Park, Seung Bum
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supporting information; experimental part
p. 151 - 154
(2012/04/04)
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- PYRIDIN-2-YL-AMINO-1,2,4-THIADIAZOLE DERIVATIVES AS GLUCOKINASE ACTIVATORS FOR THE TREATMENT OF DIABETES MELLITUS
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Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein
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Page/Page column 90-91; 94
(2009/05/29)
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- Pyrimido[5,4-e][1,2,4]triazine-5,7-diones, processes for preparing them and their use
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The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives. The invention therefore relates to compounds of the formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are suitable for use as antidiabetics, for example.
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Oxidation of aliphatic amides by N-chlorobenzenesulfonamide in acid medium catalyzed by ruthenium(III): A kinetic and mechanistic study
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The kinetics of the ruthenium(III)-catalyzed oxidation of urea and substituted ureas, namely, methylurea, ethylurea and propylurea by sodium N-chlorobenzenesulfonamide or chloramine-B (CAB) in HCI medium have been studied at 30°. The reaction rate shows a first order dependence each on [CAB], [amide] and [RuIII] and fractional order on [H+]. Additions of halide ions and the reaction product of CAB (benzenesulfonamide) and the variation of ionic strength and dielectric constant of the medium do not have any significant effect on the reaction rate. Activation parameters have been evaluated. The rate increases in D2O medium. Proton inventory studies were made in H2O-D2O mixtures for both the amides. A Taft linear free energy relationship is observed for the reaction with ρ* = -0.88 and -3.20 and δ = -0.33, indicating that electron-donating groups enhance the rate. An isokinetic relation is observed with β = 372 K confirmed by the Exner criterion. The protonation constant of monochloramine-B has been evaluated to be 8.6. A mechanism consistent with the observed kinetic data has been proposed. The rate of oxidation increases in the order: propylurea > ethylurea > methylurea > urea.
- Puttaswamy,Jagadeesha,Ramalingaiah, Hulivana
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p. 426 - 432
(2007/10/03)
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