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Lead compound from the series was tested in male Wistar rats for its effect on food intake (day and night time) and body weight. At 30 mg/Kg p. o. dose it exhibited significant reduction in food intake and body weight gain as compared to the control group. Few compounds showed activity in cognition model NORT and water maze as well. The synthesis, in-vitro binding data along with SAR and in-vivo efficacy data of the lead molecule will be presented. nl, Sylvain Celanire2, Erwin Snip1, Edith Gelens1, Remko Bakker1, Henk van der Goot1, Saskia Hulscher1, Bas-Jan Venhuis1, Michel Gillard2, Philippe Collart2, Bernard Christophe2, Benedicte Lallemand2, Florence Lebon2, Henk Timmerman1, Rob Leurs1, Patrice Talaga2, and Iwan J.

The single enantiomer 3 was initially made via an achiral Strecker amino acid synthesis and 3 was isolated from the racemic mixture after extensive chiral HPLC purification. An improved asymmetric synthesis of 3 using Evans' chiral alkylation technology will be the focus of this poster presentation. com, H Rajapakse1, M. B. Young1, P. G. Nantermet1, S. Graham1, K. Moore1, H. Selnick1, M. Stanton1, J Vacca1, Dennis Colussi2, D Hazuda2, M. T. Lai2, B. Pietrak2, E. Price2, S. Sankaranarayanan2, X.

Hack2, Nadia Nasser3, Michael P. Maher3, Hong Ao3, Anindya Bhattacharya3, Mena Kansagara3, Brian Scott4, Lin Luo3, Sandra R. Chaplan4, Alan D. Wickenden3, and J. com. (1) Department of Chemistry, Johnson & Johnson Pharmaceutical Research and Development LLC, 3210 Merryfield Row, San Diego, CA 92121, (2) Computer Aided Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development LLC, San Diego, CA 92121, (3) Pain & Related Disorders Biology, Johnson & Johnson Pharmaceutical Research and Development LLC, San Diego, CA 92121, (4) Pain & Related Disorders Biology, Johnson & Johnson Pharmaceutical Resaerch and Development LLC, San Diego, CA 92121, (5) Department of Chemistry, Johnson & Johnson Pharmaceutical Resaerch and Development LLC, San Diego, CA 92121 The transient receptor potential vanilloid 1 (TRPV1 or VR1) receptor is a ligand-gated, non-selective cation channel that is primarily expressed in nocieptive fibers.

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