912635-60-0Relevant articles and documents
A new synthesis of 4,5,6,7-Tetrahydropyrazolo[1,5-c] pyrimidines by a retro-mannich cascade rearrangement
Colombo, Raffaele,Jeon, Kyu Ok,Huryn, Donna M.,LaPorte, Matthew G.,Wipf, Peter
, p. 420 - 425 (2014/04/03)
We discovered a new retro-Mannich reaction of in situ prepared pyrazolopyridines to give pyrazolopyrimidines that have hitherto been underrepresented in the heterocyclic chemistry literature. The isolation of a linear hydrolysis product supports a mechani
Agonist lead identification for the high affinity niacin receptor GPR109a
Gharbaoui, Tawfik,Skinner, Philip J.,Shin, Young-Jun,Averbuj, Claudia,Jung, Jae-Kyu,Johnson, Benjamin R.,Duong, Tracy,Decaire, Marc,Uy, Jane,Cherrier, Martin C.,Webb, Peter J.,Tamura, Susan Y.,Zou, Ning,Rodriguez, Nathalie,Boatman, P. Douglas,Sage, Carleton R.,Lindstrom, Andrew,Xu, Jerry,Schrader, Thomas O.,Smith, Brian M.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Colletti, Steven L.,Tata, James R.,Semple, Graeme
, p. 4914 - 4919 (2008/02/12)
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.