96336-91-3Relevant academic research and scientific papers
CONDENSED PYRIDINES AND PYRIMIDINES AND THEIR USE AS ALK-5 RECEPTOR LIGANDS
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Page 22, (2010/02/07)
Therapeutically active substituted quinoline and quinazoline compounds derivatives of formula (I) wherein X is N or CH, Y is NH, N (alkyl) or NH-CH2, and R2 and R3 are specified heterorings, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor β (TGF-β), and pharmaceutical compositions for use in such therapy are disclosed.
Antifolate and antibacterial activities of 6-substituted 2,4-diaminoquinazolines
Harris, NV,Smith, C,Bowden, K
, p. 7 - 18 (2007/10/02)
6-Substituted 2,4-diaminoquinazolines (1) are good inhibitors of dihydrofolate reductase (DHFR) and effective as growth inhibitors of intact bacterial cells in vitro.The most potent compounds in the in vitro tests were, however, ineffective against a systemic murine infection.Quantitative correlations were obtained between DHFR inhibition and the substituent constant molar refractivity (MR) for 3 of the 4 enzymes studied (Escherichia coli, Streptococcus faecalis, and bovine liver DHFR); for the fourth enzyme (Staphylococcus aureus DHFR) the best correlation was obtained with a combination of MR and the lipophilic parameter ?.The recognition that the conformational properties of the 6-substituent may play a vital role in mediating the binding of 1 to DHFR prompted the synthesis of novel analogues specifically designed to test this hypothesis.From these results it was possible to construct a simple schematic model of the binding site occupied by the 6-substituents; a subsequent molecular modelling study agreed with the features of this model.
Imidazoquinazolin-2-one compounds
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, (2008/06/13)
Imidazoquinazolin-2-one compounds having platelet aggregation inhibitory activity is disclosed. These compounds have high water-solubility and reduced influences on the circulatory system and are useful for treatment and prophylaxis of intravascular throm
