69626-98-8Relevant articles and documents
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
Fernandez, Maria-Carmen,Escribano, Ana,Mateo, Ana I.,Parthasarathy, Saravanan,Martin De La Nava, Eva M.,Wang, Xiaodong,Cockerham, Sandra L.,Beyer, Thomas P.,Schmidt, Robert J.,Cao, Guoqing,Zhang, Youyan,Jones, Timothy M.,Borel, Anthony,Sweetana, Stephanie A.,Cannady, Ellen A.,Stephenson, Gregory,Frank, Scott,Mantlo, Nathan B.
scheme or table, p. 3056 - 3062 (2012/06/17)
This Letter describes the discovery and SAR optimization of 1,5-tetrahydronaphthyridines, a new class of potent CETP inhibitors. The effort led to the identification of 21b and 21d with in vitro human plasma CETP inhibitory activity in the nanomolar range (IC50 = 23 and 22 nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.
Thienopyridines. Part 4. The Preparation of Some Dithienopyridine Derivatives.
Barker, John M.,Huddleston, Patrick R.,Keenan, Guy J.
, p. 1726 - 1746 (2007/10/02)
Reaction of 6-ethoxycarbonyl-7-hydroxythienopyridin-5(4H)-one (1) with phosphoryl chloride produced the corresponding 5,7-dichloro- (2) and 7-chloro- (3) derivatives.With alkyl thioglycolate-base these led to angularly fused dithienopyridines; the nature of the products was demonstrated (through reductive dehalogenation) by correlation with dithienopyridines synthesised by an unambiguous route.
