Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
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.
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.
The phenyl ring in a series of quinolone carboxylic acid M1 positive allosteric modulators was replaced with a variety of heterocycles in order to reduce protein plasma binding and enhance CNS exposure.
Kuduk, Scott D.,Di Marco, Christina N.,Chang, Ronald K.,Ray, William J.,Ma, Lei,Wittmann, Marion,Seager, Matthew A.,Koeplinger, Kenneth A.,Thompson, Charles D.,Hartman, George D.,Bilodeau, Mark T.
scheme or table
p. 2533 - 2537
(2010/08/05)
Thienopyridines. Part 4. The Preparation of Some Dithienopyridine Derivatives.
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.
Barker, John M.,Huddleston, Patrick R.,Keenan, Guy J.
p. 1726 - 1746
(2007/10/02)
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