73027-90-4Relevant academic research and scientific papers
INDUCTION OF CELL ARREST IN G2: STRUCTURAL SPECIFICITY OF TRIGONELLINE
Lynn, David G.,Lewis, David H.,Tramontano, William A.,Evans, Lance S.
, p. 1225 - 1228 (1984)
Synthetic analogues of N-methyl nicotinic acid, trigonelline, were prepared to test the structural features necessary for the induction of cellular arrest in G2 in Pisum sativum.Analogues that (1) were regioisomers of trigonelline, (2) possessed different 1,3-substituents, ad (3) contained additional substituents on the pyridine ring were tested for their ability to induce cell arrest in G2 and to anatogize trigonelline induced arrest in G2.Only N-methyl-3-quinoline-carboxic acid and 1-methyl nicotinamide induced cell arrest in G2, and 1-methyl-4-pyridine carboxylic acid and 1-methyl-2-pyridine carboxylic acid were effective trigonelline antagonists.These data further support a specific role for trigonelline in the induction of cell arrest in G2.Key words: Pisum sativum; Leguminosae; pea; trigonelline; structural specificity; structural analogues; cell arrest; G2.
NOVEL DRUGS FOR DEMENTIA
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Example 3, (2008/06/13)
The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.
Kinetic and thermodynamic control of pseudobase formation from C-3 substituted 1-methylquinolinium cations
Bunting, John W.,Fitzgerald, Norman P.
, p. 1301 - 1307 (2007/10/02)
The kinetic and thermodynamic control of pseudobase formation from 3-W-1-methylquinolinium cations has been studied for a variety of substituents (W).Spectral data indicate that, in both aqueous and methanolic solution, the C-2 pseudobases predominate at equilibrium for W=H and Br, while the C-4 pseudobases are thermodynamically preferred species for W=CONH2, CO2CH3, CN, and NO2.Stopped-flow studies indicate that in all cases the C-2 pseudobases are the kinetically-controlled products upon basification of the aqueous solutions of these cations.Equilibrium constants (pKR+) have been measured for pseudobase formation at both C-2 and C-4 for each W in all cases where they are experimentally accessible.Substituent effects upon pK2R+ correlate with ?m for W, while pK4R+ depends upon ?-p.These substituent effects allow the prediction of pK2R+ = 15.4 and pK4R+ = 17.4 for the 1-methylquinolinium cation.Rates of C-2 to C-4 pseudobase equilibration have been measured in all cases where the latter species is thermodinamically more stable.These kinetic data allow the evaluation of rate constants for C-4 pseudobase equilibration with each cation.In all cases except W=CN, C-2 pseudobase formation is complete within the mixing time of the stopped-flow instrument.
