Advanced search×

Agonist lead identification for the high affinity niacin receptor GPR109a

Tawfik Gharbaoui, Philip J Skinner, Young-Jun Shin, Claudia Averbuj, Jae-Kyu Jung, Benjamin R Johnson, Tracy Duong, Marc Decaire, Jane Uy, Martin C Cherrier, Peter J Webb, Susan Y Tamura, Ning Zou, Nathalie Rodriguez, P Douglas Boatman, Carleton R Sage, Andrew Lindstrom, Jerry Xu, Thomas O Schrader, Brian M Smith, Ruoping Chen, Jeremy G Richman, Daniel T Connolly, Steven L Colletti, James R Tata, and Graeme Semple

Bioorg Med Chem Lett 17(17):6 (2007) PMID 17588745

A strategy for lead identification of new agonists of GPR109a is described. Early compound triage led us to 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.

DOI: 10.1016/j.bmcl.2007.06.028
Version: za2963e q8zaf q8zb5 q8zcf q8zd9 q8ze3 q8zfb q8zg0
Buy PDF

Similar articles you may find interesting…

  1. Trends in the medical management of patients with heart failure.
    Samuel W Joffe, Matthew Dewolf, and Robert J Goldberg

    J Clin Med Res 5(3):194-204 (2013) PMID 23671545

    We reviewed the medical records of 9,748 residents of the Worcester, MA, metropolitan area who were hospitalized with ADHF at all 11 central Massachusetts medical centers in 1995, 2000, 2002, and 2004. Between 1995 and 2004, respectively, the prescription upon hospital discharge of b...
    PDF not found
  2. High FDG activity in focal fat necrosis: a pitfall in interpretation of posttreatment PET/CT in patients with non-Hodgkin lymphoma.
    Raghava Kashyap, Eddie Lau, and Michael S Hofman

    Eur J Nucl Med Mol Imaging (2013) PMID 23653244

    All patients had NHL and demonstrated focal FDG-avid nodular change on CT with density higher than that of fat but lower than that of soft tissue. Histological confirmation was obtained in eight patients, with high GLUT-1 staining between necrotic tissue and organizing fat necrosis evident. Uptake r...
    Buy PDF
  3. Fast and Efficient Molecule Detection in Localization-Based Super-Resolution Microscopy by Parallel Adaptive Histogram Equalization.
    Yiming Li, Yuji Ishitsuka, and G Ulrich Nienhaus

    ACS Nano (2013) PMID 23647371

    We address the importance of reliable molecule identification for the quality of the final reconstructed super-resolution image. We present a fast and robust algorithm (a-livePALM) that vastly improves the molecule detection efficiency while minimizing false assignments that can lead to image artifa...
    Buy PDF