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Synthesis of β-carbolines from aldehydes and ketones via the α-siloxy α,β-unsaturated esters

He, Shuwen ; Lai, Zhong ; Yang, David X ; Hong, Qingmei ; Reibarkh, Mikhail ; Nargund, Ravi P ; Hagmann, William K

Tetrahedron Letters, 2010, Vol.51(33), pp.4361-4364 [Peer Reviewed Journal]

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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists

Lai, Zhong ; He, Shuwen ; Sherer, Edward C ; Wu, Zhicai ; Yu, Yang ; Ball, Richard ; Hong, Qingmei ; Yang, David X ; Guo, Liangqing ; Li, Derun ; Tuang, Quang ; Chicchi, Gary G ; Trusca, Dorina ; Tsao, Kwei-Lan ; Zhou, Yun-Ping ; Howard, Andrew D ; Nargund, Ravi P ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 01 September 2015, Vol.25(17), pp.3520-3525 [Peer Reviewed Journal]

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Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

Hong, Qingmei ; Bakshi, Raman K ; Palucki, Brenda L ; Park, Min K ; Ye, Zhixiong ; He, Shuwen ; Pollard, Patrick G ; Sebhat, Iyassu K ; Liu, Jian ; Guo, Liangqin ; Cashen, Doreen E ; Martin, William J ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Strack, Alison M ; Fong, Tung M ; Macintyre, D. Euan ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(8), pp.2330-2334 [Peer Reviewed Journal]

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Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists

Li, Derun ; Wu, Zhicai ; Yu, Yang ; Ball, Richard G ; Guo, Liangqin ; Sherer, Edward ; He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Qi, Hongbo ; Truong, Quang ; Yang, David X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Trujillo, Maria ; Pachanski, Michele ; Eiermann, George J ; Howard, Andrew D ; Zhou, Yun-Ping ; Zhang, Bei B ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.690-5 [Peer Reviewed Journal]

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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety

He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Wu, Zhicai ; Yu, Yang ; Kim, David W ; Ting, Pauline C ; Kuethe, Jeffrey T ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sperbeck, Donald M ; Sonatore, Lisa M ; Wiltsie, Judyann ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Murphy, Beth A ; Gorski, Judith N ; Liu, Jinqi ; Chen, Dunlu ; Chen, Xiaoli ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 08 August 2013, Vol.4(8), pp.773-8 [Peer Reviewed Journal]

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Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists

He, Shuwen ; Lai, Zhong ; Ye, Zhixiong ; Dobbelaar, Peter H ; Shah, Shrenik K ; Truong, Quang ; Du, Wu ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James ; Reibarkh, Mikhail ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Kerr, Janet ; Fitzgerald, Patrick ; Morissette, Pierre ; Volksdorf, Sylvia ; Eiermann, George J ; Li, Cai ; Zhang, Bei ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 10 July 2014, Vol.5(7), pp.748-53 [Peer Reviewed Journal]

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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists

He, Shuwen ; Dobbelaar, Peter H ; Guo, Liangqin ; Ye, Zhixiong ; Liu, Jian ; Jian, Tianying ; Truong, Quang ; Shah, Shrenik K ; Du, Wu ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James D ; Sherer, Edward ; Pasternak, Alexander ; Feng, Zhe ; Reibarkh, Mikhail ; Lin, Melissa ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Kerr, Janet ; Fitzgerald, Patrick ; Morissette, Pierre ; Volksdorf, Sylvia ; Eiermann, George J ; Li, Cai ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 15 March 2016, Vol.26(6), pp.1529-1535 [Peer Reviewed Journal]

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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety

He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Yang, David X ; Ting, Pauline C ; Kuethe, Jeffrey T ; Cernak, Timothy A ; Dykstra, Kevin D ; Sperbeck, Donald M ; Wu, Zhicai ; Yu, Yang ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sonatore, Lisa M ; Wiltsie, Judyann ; Liu, Jinqi ; Gorski, Judith N ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 09 October 2014, Vol.5(10), pp.1082-7 [Peer Reviewed Journal]

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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Chioda, Marc D ; Fung, Selena ; Lanza, Thomas J ; Chang, Linda ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Mclaughlin, Mark ; Belyk, Kevin M ; Krska, Shane W ; Makarewicz, Amanda K ; Martel, Elliot J ; Leone, Joseph F ; Frey, Lisa ; Karanam, Bindhu ; Madeira, Maria ; Alvaro, Raul ; Shuman, Joyce ; Salituro, Gino ; Terebetski, Jenna L ; Jochnowitz, Nina ; Mistry, Shruti ; Mcgowan, Erin ; Hajdu, Richard ; Rosenbach, Mark ; Abbadie, Catherine ; Alexander, Jessica P ; Shiao, Lin-Lin ; Sullivan, Kathleen M ; Nargund, Ravi P ; Wyvratt, Matthew J ; Lin, Linus S ; Devita, Robert J

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.717-21 [Peer Reviewed Journal]

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Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity

He, Shuwen ; Ye, Zhixiong ; Dobbelaar, Peter H ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James P ; Sebhat, Iyassu K ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Lai, Yingjie ; Franklin, Christopher L ; Reibarkh, Mikhail ; Holmes, Mark A ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Strack, Alison M ; Fong, Tung M ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(22), pp.6524-6532 [Peer Reviewed Journal]

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Discovery of potent, selective, and orally bioavailable 3 H-spiro[isobenzofuran-1,4′-piperidine] based melanocortin subtype-4 receptor agonists

Guo, Liangqin ; Ye, Zhixiong ; Liu, Jian ; He, Shuwen ; Bakshi, Raman K ; Sebhat, Iyassu K ; Dobbelaar, Peter H ; Hong, Qingmei ; Jian, Tianying ; Dellureficio, James P ; Tsou, Nancy N ; Ball, Richard G ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Chen, Howard Y ; Chen, Airu S ; Martin, William J ; Macintyre, D. Euan ; Strack, Alison M ; Fong, Tung M ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(16), pp.4895-4900 [Peer Reviewed Journal]

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Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity

He, Shuwen ; Ye, Zhixiong ; Dobbelaar, Peter H ; Sebhat, Iyassu K ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Lai, Yingjie ; Franklin, Christopher L ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Strack, Alison M ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Fong, Tung M ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 01 August 2010, Vol.20(15), pp.4399-4405 [Peer Reviewed Journal]

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Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands

Hong, Qingmei ; Bakshi, Raman K ; Dellureficio, James ; He, Shuwen ; Ye, Zhixiong ; Dobbelaar, Peter H ; Sebhat, Iyassu K ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Tang, Rui ; Kalyani, Rubana N ; Macneil, Tanya ; Vongs, Aurawan ; Rosenblum, Charles I ; Weinberg, David H ; Peng, Qingping ; Tamvakopoulos, Constantin ; Miller, Randy R ; Stearns, Ralph A ; Cashen, Doreen ; Martin, Willian J ; Chen, Airu S ; Metzger, Joseph M ; Chen, Howard Y ; Strack, Allison M ; Fong, Tung M ; Maclntyre, Euan ; Van Der Ploeg, Lex H.T ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 01 August 2010, Vol.20(15), pp.4483-4486 [Peer Reviewed Journal]

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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist

He, Shuwen ; Ye, Zhixiong ; Dobbelaar, Peter H ; Sebhat, Iyassu K ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Lai, Yingjie ; Franklin, Christopher L ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Tsou, Nancy N ; Ball, Richard G ; Cashen, Doreen E ; Martin, William J ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Strack, Alison M ; Fong, Tung M ; Macintyre, D. Euan ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(7), pp.2106-2110 [Peer Reviewed Journal]

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Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

Shah, Shrenik K ; He, Shuwen ; Guo, Liangqin ; Truong, Quang ; Qi, Hongbo ; Du, Wu ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Hong, Qingmei ; Dobbelaar, Peter ; Ye, Zhixiong ; Sherer, Edward ; Feng, Zhe ; Yu, Yang ; Wong, Frederick ; Samuel, Koppara ; Madiera, Maria ; Karanam, Bindhu V ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Feng, Yue ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Eiermann, George J ; Li, Cai ; Pachanski, Michele ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Morissette, Pierre ; Volksdorf, Sylvia ; Kerr, Janet ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Pasternak, Alexander ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 14 May 2015, Vol.6(5), pp.513-7 [Peer Reviewed Journal]

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16
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Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase

Liu, Ping ; Hamill, Terence G ; Chioda, Marc ; Chobanian, Harry ; Fung, Selena ; Guo, Yan ; Chang, Linda ; Bakshi, Raman ; Hong, Qingmei ; Dellureficio, James ; Lin, Linus S ; Abbadie, Catherine ; Alexander, Jessica ; Jin, Hong ; Mandala, Suzanne ; Shiao, Lin-Lin ; Li, Wenping ; Sanabria, Sandra ; Williams, David ; Zeng, Zhizhen ; Hajdu, Richard ; Jochnowitz, Nina ; Rosenbach, Mark ; Karanam, Bindhu ; Madeira, Maria ; Salituro, Gino ; Powell, Joyce ; Xu, Ling ; Terebetski, Jenna L ; Leone, Joseph F ; Miller, Patricia ; Cook, Jacquelynn ; Holahan, Marie ; Joshi, Aniket ; O'Malley, Stacey ; Purcell, Mona ; Posavec, Diane ; Chen, Tsing-Bau ; Riffel, Kerry ; Williams, Mangay ; Hargreaves, Richard ; Sullivan, Kathleen A ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 13 June 2013, Vol.4(6), pp.509-13 [Peer Reviewed Journal]

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17
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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes

He, Shuwen ; Ye, Zhixiong ; Truong, Quang ; Shah, Shrenik ; Du, Wu ; Guo, Liangqin ; Dobbelaar, Peter H ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James ; Pasternak, Alexander ; Feng, Zhe ; Dejesus, Reynalda ; Yang, Lihu ; Reibarkh, Mikhail ; Bradley, Scott A ; Holmes, Mark A ; Ball, Richard G ; Ruck, Rebecca T ; Huffman, Mark A ; Wong, Frederick ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Eiermann, George J ; Li, Cai ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 14 June 2012, Vol.3(6), pp.484-9 [Peer Reviewed Journal]

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18
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CCDC 780119: Experimental Crystal Structure Determination

Guoa, Liangqin ; Ye, Zhixiong ; Liu, Jian ; He, Shuwne ; Bakshi, R.K. ; Sebhat, I.K. ; Dobbelaar, P.H. ; Hong, Qingmei ; Jian, Tianying ; Dellureficio, J.P. ; Tsou, N.N. ; Ball, R.G. ; Weinberg, D.H. ; MacNeil, T. ; Tang, Rui ; Tamvakopoulos, C. ; Peng, Qianping ; Chen, H.Y. ; Chen, Airu S. ; Martin, W.J. ; MacIntyre, D.E. ; Strack, A.M. ; Fong, Tung M. ; Wyvratt, M.J. ; Nargund, R.P.

2011

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19
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Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands

Bakshi, Raman K ; Hong, Qingmei ; Tang, Rui ; Kalyani, Rubana N ; Macneil, Tanya ; Weinberg, David H ; Van Der Ploeg, Lex H.T ; Patchett, Arthur A ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(5), pp.1130-1133 [Peer Reviewed Journal]

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20
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CCDC 881690: Experimental Crystal Structure Determination

He, Shuwen ; Ye, Zhixiong ; Truong, Quang ; Shah, Shrenik ; Du, Wu ; Guo, Liangqin ; Dobbelaar, P.H. ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Qi, Hongbo ; Bakshi, R.K. ; Hong, Qingmei ; Dellureficio, J. ; Pasternak, A. ; Feng, Zhe ; deJesus, R. ; Yang, L. ; Reibarkh, M. ; Bradley, S.A. ; Holmes, M.A. ; Ball, R.G. ; Ruck, R.T. ; Huffman, M.A. ; Wong, F. ; Samuel, K. ; Reddy, V.B. ; Mitelman, S. ; Tong, S.X. ; Chicchi, G.G. ; Tsao, Kwei-Han ; Trusca, D. ; Wu, M. ; Shao, Qing ; Trujillo, M. ; Eiermann, G.J. ; Li, Cai ; Zhang, Bei ; Howard, A.D. ; Zhou, Yun-Ping ; Nargund, R.P. ; Hagmann, W.K.

2012

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21
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CCDC 760573: Experimental Crystal Structure Determination

He, Shuwen ; Ye, Zhixiong ; Dobbelaar, P.H. ; Sebhat, I.K. ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Lai, Yingjie ; Franklin, C.L. ; Bakshi, R.K. ; Dellureficio, J.P. ; Hong, Qingmei ; Tsou, N.N. ; Ball, R.G. ; Cashen, D.E. ; Martin, W.J. ; Weinberg, D.H. ; MacNeil, T. ; Tang, Rui ; Tamvakopoulos, C. ; Peng, Qianping ; Miller, R.R. ; Stearns, R.A. ; Chen, H.Y. ; Chen, A.S. ; Strack, A.M. ; Fong, T.M. ; MacIntyre, D.E. ; Wyvratt Junior, M.J. ; Nargund, R.P.

2010

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22
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1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: Application in the synthesis of potent human melanocortin-4 receptor selective agonists

Bakshi, Raman K ; Hong, Qingmei ; Olson, J.T ; Ye, Zhixiong ; Sebhat, Iyassue K ; Weinberg, David H ; Macneil, Tanya ; Kalyani, Rubana N ; Tang, Rui ; Martin, William J ; Strack, Alison ; Mcgowan, Erin ; Tamvakopoulos, Constantin ; Miller, Randy R ; Stearns, Ralph A ; Tang, Wei ; Maclntyre, D. Euan ; van Der Ploeg, Lex H.T ; Patchett, Arthur A ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(14), pp.3430-3433 [Peer Reviewed Journal]

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Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC)

Yu, Yang ; Wu, Zhicai ; Shi, Zhi-Cai ; He, Shuwen ; Lai, Zhong ; Cernak, Timothy A ; Vachal, Petr ; Liu, Min ; Liu, Jian ; Hong, Qingmei ; Jian, Tianying ; Guiadeen, Deodial ; Krikorian, Arto ; Sperbeck, Donald M ; Verras, Andreas ; Sonatore, Lisa M ; Murphy, Beth A ; Wiltsie, Judyann ; Chung, Christine C ; Gorski, Judith N ; Liu, Jinqi ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; De Vita, Robert J ; Pinto, Shirly ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 01 June 2019, Vol.29(11), pp.1380-1385 [Peer Reviewed Journal]

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Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety

He, Shuwen ; Lai, Zhong ; Hong, Qingmei ; Shang, Jackie ; Reibarkh, Mikhail ; Kuethe, Jeffrey T ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Cernak, Timothy A ; Dykstra, Kevin D ; Sperbeck, Donald M ; Wu, Zhicai ; Yu, Yang ; Yang, Ginger X ; Jian, Tianying ; Verras, Andreas ; Sonatore, Lisa M ; Wiltsie, Judyann ; Chung, Christine C ; Murphy, Beth A ; Gorski, Judith N ; Liu, Jinqi ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 15 May 2019, Vol.29(10), pp.1182-1186 [Peer Reviewed Journal]

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