Matthew Gregory Bursavich
Pfizer
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Publication
Featured researches published by Matthew Gregory Bursavich.
Bioorganic & Medicinal Chemistry Letters | 2011
Adam M. Gilbert; Matthew Gregory Bursavich; Sabrina Lombardi; Adedayo Adedoyin; Jason M. Dwyer; Zoë A. Hughes; Jeffrey Curtis Kern; Xavier Khawaja; Sharon Rosenzweig-Lipson; William J. Moore; Sarah Neal; Michael Olsen; Stacey J. Sukoff Rizzo; Dane Springer
A series of 3-(pyridin-2-yl-ethynyl)benzamide negative allosteric modulators of the metabotropic glutamate receptor 5 (mGluR5 NAMs) have been prepared. Starting from HTS hit 1 (IC(50): 926 nM), potent mGluR5 NAMs showing excellent potencies (IC(50)s<50 nM) and good physicochemical profiles were prepared by monitoring LipE values. One compound 26 showed excellent mGluR5 binding (K(i): 21 nM) and antagonism (IC(50): 8 nM), an excellent rat PK profile (CL: 12 mL/min/kg, %F: 85) and showed oral activity in a mouse 4-Plate Behavioral model of anxiety (MED: 30 mpk) and a mouse Stress Induced Hyperthermia model of anxiety (MED 17.8 mpk).
Archive | 2008
Arie Zask; Pawel Wojciech Nowak; Jeroen C. Verheijen; Kevin J. Curran; Joshua Kaplan; David Malwitz; Matthew Gregory Bursavich; Derek Cecil Cole; Semiramis Ayral-Kaloustian; Ker Yu; David J. Richard; Mark Lefever
Archive | 2005
Fuk-Wah Sum; Dennis Powell; Yixian Zhang; Lijing Chen; Scott Lee Kincaid; Lee D. Jennings; Yongbo Hu; Adam M. Gilbert; Matthew Gregory Bursavich
Archive | 2008
Matthew Gregory Bursavich; Aranapakam Mudumbai Venkatesan; Pawel Wojciech Nowak; Sabrina Lombardi; Adam M. Gilbert; Christoph Martin Denhardt; Osvaldo Dos Santos; Efren Delos Santos; Natasja Brooijmans; Semiramis Ayral-Kaloustian; Zecheng Chen; Jeroen C. Verheijen; Joshua Kaplan; Arie Zask
Archive | 2005
Fuk-Wah Sum; Dennis Powell; Yixian Zhang; Lijing Chen; Scott Lee Kincaid; Lee D. Jennings; Yongbo Hu; Adam M. Gilbert; Matthew Gregory Bursavich
Archive | 2009
Matthew Gregory Bursavich; Adam M. Gilbert; Joseph Raymond Stock
Archive | 2008
Matthew Gregory Bursavich; Adam M. Gilbert; Diane B. Hauze; Charles William Mann; Jeffrey C. Pelletier
Archive | 2009
Matthew Gregory Bursavich; Nan Zhang; Semiramis Ayral-Kaloustian; James T. Anderson; Thai Hiep Nguyen; Sabrina Lombardi; David Malwitz; Natasja Brooijmans; Derek Cecil Cole; Adam M. Gilbert; Pawel Wojciech Nowak; Kaapjoo Park; Sasmita Das; Hwei-Ru Tsou; Aranapakam Mudumbai Venkatesan; Mercy Adufa Otteng; Gary Harold Birnberg; Gloria Jean Macewan
Archive | 2009
Hwei-Ru Tsou; Gary Harold Birnberg; Gloria Jean Macewan; Semiramis Ayral-Kaloustian; Matthew Gregory Bursavich; Sabrina Lombardi; Nan Zhang; Adam M. Gilbert; George Theordore Grosu; Natasja Brooijmans; Thai Hiep Nguyen
Archive | 2008
Diane B. Hauze; Matthew Gregory Bursavich; Luciana de Araujo Felix; Adam M. Gilbert; Jeffrey C. Pelletier
