Publications

Select publications:

Research Articles

1.  Identification and characterization of sebaceous gland atrophy-sparing DGAT1 inhibitors. Muise, E.S.; Zhu, Y.; Verras, A.; Karanam, B.V.; Gorski, J.; Weingarth, D.; Lin, H.V.; Hwa, J.; Thompson, J.R.; Hu, G.; Liu, J.; He, S.; DeVita, R.J.; Shen, D.-M.; Pinto, S. PLoS One 2014, 9(2), e88908/1-e88908/12, 12 pp.

2. Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain, Chobanian, H.R.; Guo, Y.; Liu, P.; Chioda, M.D.; Fung, S.; Lanza, T.J.; Chang, L.; Bakshi, R.K.; Dellureficio, J.P.; Hong, Q.; McLaughlin, M.; Belyk, K.M.; Krska, S.W.; Makarewicz, A.K.; Martel, E.J.; Leone, J.F.; Frey, L.; Karanam, B.; Madeira,M.; Alvaro, R.; Shuman, J.; Salituro, G.; Terebetski, J.L.; Jochnowitz, N.; Mistry, S.; McGowan, E.; Hajdu, R.; Rosenbach, M.; Abbadie, C.; Alexander, J.P.; Shiao, L.-L.; Sullivan, K.M.; Nargund, R.P.; Wyvratt, M.J.; Linus S. Lin, L.S.; and DeVita, R.J.  ACS Med. Chem. Lett., 2014, 5(6), 717-721. DOI:10.1021/ml5001239.

3. Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety, He, S.; Hong, Q.; Lai, Z.; Yang, D.X.; Tong, P.C.; Kuethe, J.T.; Cernak, T.C.; Dykstra, K.D.; Sperbeck, D.M.; Wu, Z.; Yu, Y.; Yang, G.X.; Jian, T.; Liu, J.; Guiadeen, D.; Krikorian, A.D.; Sonatore, L.M.; Wiltsie, J.; Liu, J.; Gorski, J.N.; Chung, C.C.; Gibson, J.T.; Lisnock, J.; Xiao, J.; Wolff, M.; Tong, S.X.; Madeira, M.; Karanam, B.V.; Shen, D.-M.; Balkovec, J.M; Pinto, S.; Nargund, R.P.; DeVita, R.J. ACS Med. Chem. Lett., 2014, 5 (10), pp 1082–1087.

4. Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase. Liu, P.; Hamill, T.G.; Chioda, M.; Chobanian, H.; Fung, S.; Guo, Y.; Chang, L.; Bakshi, R.; Hong, Q.; Dellureficio, J.; Lin, L.S.; Abbadie, C.; Alexander, J.; Jin, H.; Mandala, S.; Shiao, L.-L.; Li, W.; Sanabria, S.; Williams, D.; Zeng, Z.; Hajdu, R.; Jochnowitz, N.; Rosenbach, M.; Karanam, B.; Madeira, M.; Salituro, G.; Powell, J.; Xu, L.; Terebetski, J.L.; Leone, J.F.; Miller, P.; Cook, J.; Holahan, M.; Joshi, A.; O’Malley, S.; Purcell, M.; Posavec, D.; Chen, T.-B.; Riffel, K.; Williams, M.; Hargreaves, R.; Sullivan, K.A.; Nargund, R.P.; DeVita, R.J. ACS Med. Chem. Lett. 2013, 509-513.

5. Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety, He, S.; Hong, Q.; Lai, Z.; Wu, Z.; Yu, Y.; Kim, D.W.; Ting, P.C.; Kuethe, J.T.; Yang, G.X.; Jian, T.; Liu, J.; Guiadeen, D.; Krikorian, A.D.; Sperbeck, D.M.; Sonatore, L.M.; Wiltsie, J.; Chung, C.C.; Gibson, J.T.; Lisnock, J.; Murphy, B.A.; Gorski, J.N.; Liu, J.; Chen, D.; Chen, X.; Wolff, M.; Tong, S.X.; Madeira, M.; Karanam, B.V.; Shen, D.-M.; Balkovec, J.M; Pinto, S.; Nargund, R.P.; DeVita, R.J. ACS Med. Chem. Lett., 2013, 773-778.

6. 2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)-octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: A Potent Human NK1 Receptor Antagonist with Multiple Clearance Pathways, Kassick, A.J.; Jiang, J.; Bunda, J.; Wilson, D.; Bao, J.; Lu, H.; Ball, R.G.; Doss, G.A.; Tong, X.; Tsao, K.-L.C.; Wang, H.; Chicchi, G.; Karanam, B.; Tschirret-Guth, R.; Samuel, K.; Hora, D.F.; Kumar, S.; Madeira, M.; Eng, W.; Hargreaves, R.; Purcell, M.; Gantert, L.; Cook, J.; DeVita, R.J.; Mills, S.G. J. Med.Chem. 2013, 5940-5948.

 

7. Synthesis of Oxaspiropiperidines as a Strategy for Lowering logD, Cernak*, T.; Kevin Dykstra, K; Levorse, D.; Verras, A.; Balkovec, J.; Nargund, R.; DeVita, R. J..; Tetrahedron Letters, 2011, 6457-6459.

Reviews and Persectives

1.  Current Status of the Research and Development of DGAT1 Inhibitors, DeVita, R.J.; Pinto, S.  J. Med.Chem. 2013, 56 (24), pp 9820–9825. Invited perspective,  DOI: 10.1021/jm4007033

2. The Changing Drug Discovery Paradigm, DeVita, R.J.; Wuelfing, W.P., McGregor, C.; Bak, A.  American Association of Pharmaceutical Science News Magazine, 2012, July issue, 20-23.