Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Andres S, Hernandez"'
Autor:
Dawn Sun, James Kempson, Peng Li, Dauh-Rurng Wu, Arvind Mathur, Huiping Zhang, Shiuhang Henry Yip, Andres S. Hernandez
Publikováno v:
SEPARATION SCIENCE PLUS. 2:343-352
Autor:
Jeffrey A. Robl, Michael Thomas, Mary Ann Pelleymounter, Brian Gemzik, Anthony V. Azzara, Brian J. Murphy, Sharon N. Bisaha, Helen E. Godonis, Daniel Longhi, Neil Flynn, William N. Washburn, Kenneth W. Rohrbach, Khehyong Ngu, Saleem Ahmad, Susan Harvey, Christine Huang, Evan B. Janovitz, Andres S. Hernandez, James Devenny, Hongwei Zhang, Lisa Zhang, Susan Glick, Suzanne Rooney, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8848-8858
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Autor:
Gary G. Cao, Min Zhou, Ramya Jayaram, Douglas B. Moore, Andres S. Hernandez, Tao Wang, Jean M. Whaley, Yue-Zhong Shu, Carrie Xu, Lori Kunselman, Atsu Apedo, William R. Ewing, Reshma Panemangalore, Qi Gao, Arvind Mathur, Richard Rampulla, Bradley A. Zinker, Lauren Haque, Mary Ellen Cvijic, Marta Dabros, Arun Kumar Gupta, Heng Liu, Jeffrey A. Robl, Bruce A. Ellsworth, Jun Shi, Zhengxiang Gu, Jason J. Wilkes, Akin H. Davulcu, Kristin N. Williams, Elizabeth A. Dierks, John Krupinski, Zhenqiu Hong, Edward J. Brady, Ximao Wu, Qin Sun, Hong Cai, Chunshan Xie, Elizabeth A. Jurica, Kimberly A. Foster
Publikováno v:
Journal of medicinal chemistry. 61(3)
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GP
Autor:
Neil Flynn, Mary Jane Cullen, Hongwei Zhang, Wei Wang, Susan Glick, Lisa Zhang, Jeffrey A. Robl, Pratik Devasthale, Andres S. Hernandez, Christian Caporuscio, Brian J. Murphy, Suzanne Rooney, Ning Huang, Mary Ann Pelleymounter, Kenneth W. Rohrbach, Kishore Renduchintala, Anthony V. Azzara, Helen E. Godonis, Yi-Xin Li, Radhakrishnan Sridhar, Michael Thomas, Susan Harvey, Paul Stetsko, Mary F. Grubb, Chris Freeden, Fang Moore, Christine Huang, James Devenny, Daniel Longhi, William N. Washburn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2793-2799
Our investigation of the structure–activity and structure–liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can i
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Autor:
William R. Ewing, Carrie Xu, Heng Liu, Brian J. Murphy, Neil Flynn, Tao Wang, Douglas B. Moore, Lori Kunselman, Bruce A. Ellsworth, Elizabeth A. Jurica, Kimberly A. Foster, Atsu Apedo, Yuan Tian, Yang Hong, Arvind Mathur, Bradley A. Zinker, Biji Jacob, Kristin N. Williams, Min Zhou, Brad D. Maxwell, Gary Cao, Andres S. Hernandez, Qin Sun, Hong Cai, Jean M. Whaley, Elizabeth A. Dierks, Joel C. Barrish, Dora M. Schnur, Ximao Wu, Doree F. Sitkoff, Mary Ellen Cvijic, Richard Rampulla, Chunshan Xie, David S. Nirschl, Reshma Panemangalore, Michael B. Hicks, Jeffrey A. Robl, Jason J. Wilkes
Publikováno v:
Journal of medicinal chemistry. 60(4)
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-
Autor:
Jeffrey A. Robl, Guohua Zhao, Joel C. Barrish, Bei Wang, Brad D. Maxwell, Christian Caporuscio, Hongwei Zhang, James Devenny, Mary F. Grubb, Zhenghua Wang, Suzanne Rooney, James Mignone, Lisa Zhang, Brian J. Murphy, Wei Wang, Daniel Longhi, William N. Washburn, Kenneth W. Rohrbach, Evan B. Janovitz, Mark C. Manfredi, Mary Ann Pelleymounter, Michael Thomas, Hong Yang, Paul Stetsko, Saleem Ahmad, Atsu Apedo, Mary Jane Cullen, Brian Gemzik, Ning Huang, Chris Freeden, Susan Harvey, Anthony V. Azzara, Khehyong Ngu, Christine Huang, Rulin Zhao, Susan Glick, Neil Flynn, Pratik Devasthale, Andres S. Hernandez, Helen E. Godonis
Publikováno v:
Journal of Medicinal Chemistry. 57:7509-7522
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high affinity allowed us
Autor:
Saleem, Ahmad, William N, Washburn, Andres S, Hernandez, Sharon, Bisaha, Khehyong, Ngu, Wei, Wang, Mary Ann, Pelleymounter, Daniel, Longhi, Neil, Flynn, Anthony V, Azzara, Kenneth, Rohrbach, James, Devenny, Suzanne, Rooney, Michael, Thomas, Susan, Glick, Helen, Godonis, Susan, Harvey, Hongwei, Zhang, Brian, Gemzik, Evan B, Janovitz, Christine, Huang, Lisa, Zhang, Jeffrey A, Robl, Brian J, Murphy
Publikováno v:
Journal of medicinal chemistry. 59(19)
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Discovery, synthesis, and structure–activity studies of tetrazole based growth hormone secretagogues
Autor:
David A. Gordon, Christa M. Musial, R. Krishna Seethala, Leah Giupponi, Kenneth E.J. Dickinson, Jeffrey A. Robl, Peter T. W. Cheng, Neil Flynn, Mark A. Smith, Dorothy Slusarchyk, Joseph A. Tino, Brian J. Murphy, Stephen G. Swartz, Gary J. Grover, Andres S. Hernandez, R.J. George, Daniel Longhi, Scott A. Biller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5928-5933
A novel class of Growth Hormone Secretagogues (GHS), based on a tetrazole template, has been discovered. In vitro SAR and in vivo potency within this new class of GHS are described. The tetrazole 9q exhibits good oral bioavailability in rats and dogs
Autor:
Jun Li, Lawrence J. Kennedy, Shung Wu, Carrie Xu, Hossain Monshizadegan, Stanley R. Krystek, Robert Zahler, Thomas Harrity, Huiping Zhang, Daniel Meyers, Debra Search, Yongmi An, Chiehying Chang, Rebecca A. Smirk, Michael Cap, Rongan Zhang, Shiwei Tao, Bang-Chi Chen, Ngiap-Kie Lim, Hao Zhang, Peter T. W. Cheng, Litao Zhang, Lori Kunselman, Stephanie Y. Chen, Pratik Devasthale, Pathanjali Kadiyala, Andres S. Hernandez, Michael A. Blanar, Joseph A. Tino, Ranjan Mukherjee, Ying Wang, Xiang-Yang Ye, Chen Sean, Yan Shi, Kevin O’Malley, Bowman Miao, Scott A. Bolton, Zhi Lai, Rai Ajit Srivastava, Wei Wang, Vinayak Hosagrahara, Kenneth T. Locke, Denis E. Ryono, Denise Grimm, Lisa Zhang, Jodi K. Muckelbauer, Yi-Xin Li
Publikováno v:
Journal of medicinal chemistry. 53(7)
An 1,3-oxybenzylglycine based compound 2 (BMS-687453) was discovered to be a potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs h
Autor:
Samantha Gagne, Brian J. Murphy, Soratree Charoenthongtrakul, Brad J. Geddes, Elizabeth K. Govek, Neil Flynn, Derek J. Giuliana, Kristen Morgan, Kenneth A. Longo, Andres S. Hernandez, Peter S. DiStefano, Joseph A. Tino, Jun Li, David A. Gordon, Anna Nolan, Jeffrey Hixon
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 329(3)
The orexigenic peptide ghrelin has been shown to have prokinetic activity in the gastrointestinal (GI) system of several species, including humans. In this series of experiments, we have evaluated the prokinetic activity of novel, small-molecule ghre