347393-41-3Relevant academic research and scientific papers
Synthesis, molecular modelling and biological studies of 3-hydroxy-pyrane-4-one and 3-hydroxy-pyridine-4-one derivatives as HIV-1 integrase inhibitors
Sirous, Hajar,Fassihi, Afshin,Brogi, Simone,Campiani, Giuseppe,Christ, Frauke,Debyser, Zeger,Gemma, Sandra,Butini, Stefania,Chemi, Giulia,Grillo, Alessandro,Zabihollahi, Rezvan,Aghasadeghi, Mohammad R.,Saghaie, Lotfollah,Memarian, Hamid R.
, p. 755 - 770 (2019/11/02)
Background: Despite the progress in the discovery of antiretroviral compounds for treating HIV-1 infection by targeting HIV integrase (IN), a promising and well-known drug target against HIV-1, there is a growing need to increase the armamentarium against
Synthesis of 2-amido-3-hydroxypyridin-4(1H)-ones: Novel iron chelators with enhanced pFe3+ values
Liu, Zu D.,Piyamongkol,Liu, Ding Y.,Khodr, Hicham H.,Lu, Shu L.,Hider, Robert C.
, p. 563 - 573 (2007/10/03)
The synthesis of a range of 2-amido-3-hydroxypyridin-4-ones as bidentate iron(III) chelators with potential for oral administration is described. The pKa values of the ligands together with the stability constants of their iron(III) complexes have been determined. Results indicate that the introduction of an amido substituent at the 2-position leads to an appreciable enhancement of the pFe3+ values. The ability of these novel 3-hydroxypyridin-4-ones to facilitate the iron excretion in bile was investigated using a 59Fe-ferritin loaded rat model. The optimal effect was observed with the N-methyl amido derivative 15b, which has an associated pFe3+ value of 21.7, more than two orders of magnitude higher than that of deferiprone (1,2-dimethyl-3-hydroxypyridin-4-one) 1a (pFe3+=19.4). Dose response studies suggest that chelators with high pFe3+ values scavenge iron more effectively at lower doses when compared with simple dialkyl substituted hydroxypyridinones. Copyright
