321744-26-7Relevant articles and documents
The discovery of CCR3/H1 dual antagonists with reduced hERG risk
Barton, Patrick,Brough, Steven,Evans, Richard,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Rigby, Aaron,Sanganee, Hitesh,Sisson, Adam,Springthorpe, Brian,Bahl, Ash,Bowers, Keith,Riley, Robert J.
, p. 6688 - 6693,6 (2012/12/12)
A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to del
Synthesis of all isomers of pulcherrimine, a bitter principle in the sea urchin ovary
Sata, Noriko U,Kuwahara, Ryuji,Murata, Yuko
, p. 115 - 118 (2007/10/03)
All eight isomers of pulcherrimine, a bitter principle of the sea urchin (Hemicentrotus pulcherrimus) ovary have been synthesized, which led to revision of the absolute stereochemistry of pulcherrimine. The synthetic pulcherrimine and the 2S isomer were highly bitter at a concentration of 1.0 mM.
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid
Bellier, Bruno,Da Nascimento, Sophie,Meudal, Herve,Gincel, Edith,Roques, Bernard P.,Garbay, Christiane
, p. 1419 - 1424 (2007/10/03)
A new series of 4-substituted pipecolic acid derivatives was prepared and incorporated into dipeptoids. The resulting products behave as moderately potent CCK-B antagonists but their constrained structure and its comparison with structurally related compounds yield valuable information about the conformational requirements for optimal recognition of the CCK-B receptor by antagonists.