138642-48-5Relevant articles and documents
Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials
Yeates, Clive L.,Batchelor, John F.,Capon, Edward C.,Cheesman, Neil J.,Fry, Mitch,Hudson, Alan T.,Pudney, Mary,Trimming, Helen,Woolven, James,Bueno, José M.,Chicharro, Jesús,Fernández, Esther,Fiandor, José M.,Gargallo-Viola, Domingo,De Las Heras, Federico Gómez,Herreros, Esperanza,León, María L.
, p. 2845 - 2852 (2008/12/23)
A series of diaryl ether substituted 4-pyridones have been identified as having potent antimalarial activity superior to that of chloroquine against Plasmodium falciparum in vitro and murine Plasmodium yoelii in vivo. These were derived from the anticoccidial drug clopidol through a systematic study of the effects of varying the side chain on activity. Relative to clopidol the most active compounds show > 500-fold improvement in IC50 for inhibition of P. falciparum in vitro and about 100-fold improvement with respect to ED50 against P. yoelii in mice. These compounds have been shown elsewhere to act selectively by inhibition of mitochondrial electron transport at the cytochrome bc1 complex.
New Nonpeptide Angiotensin II Receptor Antagonists> 3. Synthesis, Biological Properties, and Structure-Activity Relationships of 2-Alkyl-4-(biphenylylmethoxy)pyridine Derivatives
Bradbury, Robert H.,Allott, Christopher P.,Dennis, Michael,Girdwood, J. Alan,Kenny, Peter W.,et al.
, p. 1245 - 1254 (2007/10/02)
A novel series of nonpeptide angiotensin II (AII) receptor antagonists is reported, derived from linkage of the biphenylyltetrazole moiety found in previously described antagonists via a methyleneoxy chain to the 4-position of a 3-substituted 2,6-dialkylp
