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5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors

Arasappan, Ashok ; Bennett, Frank ; Girijavallabhan, Vinay ; Huang, Yuhua ; Huelgas, Regina ; Alvarez, Carmen ; Chen, Lei ; Gavalas, Stephen ; Kim, Seong-Heon ; Kosinski, Aneta ; Pinto, Patrick ; Rizvi, Razia ; Rossman, Randall ; Shankar, Bandarpalle ; Tong, Ling ; Velazquez, Francisco ; Venkatraman, Srikanth ; Verma, Vishal A ; Kozlowski, Joseph ; Shih, Neng-Yang ; Piwinski, John J ; Maccoss, Malcolm ; Kwong, Cecil D ; Clark, Jeremy L ; Fowler, Anita T ; Geng, Feng ; Kezar, Hollis S ; Roychowdhury, Abhijit ; Reynolds, Robert C ; Maddry, Joseph A ; Ananthan, Subramaniam ; Secrist, John A ; Li, Cheng ; Chase, Robert ; Curry, Stephanie ; Huang, Hsueh-Cheng ; Tong, Xiao ; Njoroge, F George

Bioorganic & medicinal chemistry letters, 01 May 2012, Vol.22(9), pp.3229-34 [Peer Reviewed Journal]

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Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors

Bennett, Frank ; Kezar, Hollis S ; Girijavallabhan, Vinay ; Huang, Yuhua ; Huelgas, Regina ; Rossman, Randall ; Shih, Neng-Yang ; Piwinski, John J ; Maccoss, Malcolm ; Kwong, Cecil D ; Clark, Jeremy L ; Fowler, Anita T ; Geng, Feng ; Roychowdhury, Abhijit ; Reynolds, Robert C ; Maddry, Joseph A ; Ananthan, Subramaniam ; Secrist, John A ; Li, Cheng ; Chase, Robert ; Curry, Stephanie ; Huang, Hsueh-Cheng ; Tong, Xiao ; George Njoroge, F ; Arasappan, Ashok

Bioorganic & medicinal chemistry letters, 01 August 2012, Vol.22(15), pp.5144-9 [Peer Reviewed Journal]

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Synthesis and biological evaluation of 5R- and 5S-methyl substituted d- and l-configuration 1,3-dioxolane nucleoside analogs

Bera, Sanjib ; Malik, Leila ; Bhat, Balkrishen ; Carroll, Steven S ; Hrin, Renee ; Maccoss, Malcolm ; Mcmasters, Daniel R ; Miller, Michael D ; Moyer, Greg ; Olsen, David B ; Schleif, William A ; Tomassini, Joanne E ; Eldrup, Anne B

Bioorganic & Medicinal Chemistry, 01 December 2004, Vol.12(23), pp.6237-6247 [Peer Reviewed Journal]

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Synthesis and evaluation of optically pure dioxolanes as inhibitors of hepatitis C virus RNA replication

Bera, Sanjib ; Malik, Leila ; Bhat, Balkrishen ; Carroll, Steven S ; Maccoss, Malcolm ; Olsen, David B ; Tomassini, Joanne E ; Eldrup, Anne B

Bioorganic & Medicinal Chemistry Letters, 15 December 2003, Vol.13(24), pp.4455-4458 [Peer Reviewed Journal]

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4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties

Butora, Gabor ; Morriello, Gregori J ; Kothandaraman, Shankaran ; Guiadeen, Deodialsingh ; Pasternak, Alexander ; Parsons, William H ; Maccoss, Malcolm ; Vicario, Pasquale P ; Cascieri, Margaret A ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 15 September 2006, Vol.16(18), pp.4715-4722 [Peer Reviewed Journal]

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Synthesis and HCV inhibitory properties of 9-deaza- and 7,9-dideaza-7-oxa-2′- C-methyladenosine

Butora, Gabor ; Olsen, David B ; Carroll, Steven S ; Mcmasters, Daniel R ; Schmitt, Christoph ; Leone, Joseph F ; Stahlhut, Mark ; Burlein, Christine ; Maccoss, Malcolm

Bioorganic & Medicinal Chemistry, 2007, Vol.15(15), pp.5219-5229 [Peer Reviewed Journal]

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The elusive 8-fluoroadenosine: a simple non-enzymatic synthesis and characterization

Butora, Gabor ; Schmitt, Christoph ; Levorse, Dorothy A ; Streckfuss, Eric ; Doss, George A ; Maccoss, Malcolm

Tetrahedron, 2007, Vol.63(18), pp.3782-3789 [Peer Reviewed Journal]

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Administration of a HepDirect™ Prodrug of 2′-C-methylcytidine to Hepatitis C Virus Infected Chimpanzees

Carroll, Steven ; Koeplinger, Kenneth ; Vavrek, Marissa ; Handt, Laurence ; Maccoss, Malcolm ; Hecker, Scott ; Olsen, David

Antiviral Research, May 2009, Vol.82(2), pp.A22-A22 [Peer Reviewed Journal]

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Antiviral efficacy upon administration of a HepDirect prodrug of 2'-C-methylcytidine to hepatitis C virus-infected chimpanzees

Carroll, Steven S ; Koeplinger, Kenneth ; Vavrek, Marissa ; Zhang, Nanyan Rena ; Handt, Laurence ; Maccoss, Malcolm ; Olsen, David B ; Reddy, K Raja ; Sun, Zhili ; Van Poelje, Paul D ; Fujitaki, James M ; Boyer, Serge H ; Linemeyer, David L ; Hecker, Scott J ; Erion, Mark D

Antimicrobial agents and chemotherapy, August 2011, Vol.55(8), pp.3854-60 [Peer Reviewed Journal]

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Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees

Carroll, Steven S ; Ludmerer, Steven ; Handt, Larry ; Koeplinger, Kenneth ; Zhang, Nanyan Rena ; Graham, Donald ; Davies, Mary-Ellen ; Maccoss, Malcolm ; Hazuda, Daria ; Olsen, David B

Antimicrobial agents and chemotherapy, March 2009, Vol.53(3), pp.926-34 [Peer Reviewed Journal]

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Inhibition of hepatitis C virus RNA replication by 2'-modified nucleoside analogs

Carroll, Steven S ; Tomassini, Joanne E ; Bosserman, Michele ; Getty, Krista ; Stahlhut, Mark W ; Eldrup, Anne B ; Bhat, Balkrishen ; Hall, Dawn ; Simcoe, Amy L ; Lafemina, Robert ; Rutkowski, Carrie A ; Wolanski, Bohdan ; Yang, Zhucheng ; Migliaccio, Giovanni ; De Francesco, Raffaele ; Kuo, Lawrence C ; Maccoss, Malcolm ; Olsen, David B

The Journal of biological chemistry, 04 April 2003, Vol.278(14), pp.11979-84 [Peer Reviewed Journal]

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Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket

Castonguay, Laurie A ; Weng, Youmin ; Adolfsen, William ; Di Salvo, Jerry ; Kilburn, Ruth ; Caldwell, Charles G ; Daugherty, Bruce L ; Finke, Paul E ; Hale, Jeffrey J ; Lynch, Christopher L ; Mills, Sander G ; Maccoss, Malcolm ; Springer, Martin S ; Demartino, Julie A

Biochemistry, 18 February 2003, Vol.42(6), pp.1544-50 [Peer Reviewed Journal]

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Substituted Imidazoles as Glucagon Receptor Antagonists

Chang, Linda L ; Sidler, Kelly L ; Cascieri, Margaret A ; de Laszlo, Stephen ; Koch, Greg ; Li, Bing ; Maccoss, Malcolm ; Mantlo, Nathan ; O'Keefe, Stephen ; Pang, Margaret ; Rolando, Anna ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(18), pp.2549-2553 [Peer Reviewed Journal]

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Highly constrained bicyclic VLA-4 antagonists

Chang, Linda L ; Truong, Quang ; Doss, George A ; Maccoss, Malcolm ; Lyons, Kathryn ; Mccauley, Ermengilda ; Mumford, Richard ; Forrest, Gail ; Vincent, Stella ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(3), pp.597-601 [Peer Reviewed Journal]

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The discovery of small molecule carbamates as potent dual α 4β 1/α 4β 7 integrin antagonists

Chang, Linda L ; Truong, Quang ; Mumford, Richard A ; Egger, Linda A ; Kidambi, Usha ; Lyons, Kathryn ; Mccauley, Ermengilda ; Van Riper, Gail ; Vincent, Stella ; Schmidt, John A ; Maccoss, Malcolm ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(2), pp.159-163 [Peer Reviewed Journal]

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16
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Orally active inhibitors of stromelysin-1 (MMP-3)

Chapman, Kevin T ; Durette, Philippe L ; Caldwell, Charles G ; Sperow, Kelly M ; Niedzwiecki, Lisa M ; Harrison, Richard K ; Saphos, Cheryl ; Christen, Amy J ; Olszewski, Julie M ; Moore, Vernon L ; Maccoss, Malcolm ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(7), pp.803-806 [Peer Reviewed Journal]

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17
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Potent, orally absorbed glucagon receptor antagonists

de Laszlo, Stephen E ; Hacker, Candice ; Li, Bing ; Kim, Dooseop ; Maccoss, Malcolm ; Mantlo, Nathan ; Pivnichny, James V ; Colwell, Larry ; Koch, Gregory E ; Cascieri, Margaret A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 1999, Vol.9(5), pp.641-646 [Peer Reviewed Journal]

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18
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Pyrroles and other heterocycles as inhibitors of P38 kinase

de Laszlo, Stephen E ; Visco, Denise ; Agarwal, Lily ; Chang, Linda ; Chin, Jayne ; Croft, Gist ; Forsyth, Amy ; Fletcher, Daniel ; Frantz, Betsy ; Hacker, Candice ; Hanlon, William ; Harper, Coral ; Kostura, Matthew ; Li, Bing ; Luell, Sylvie ; Maccoss, Malcolm ; Mantlo, Nathan ; O'Neill, Edward A ; Orevillo, Chad ; Pang, Margaret ; Parsons, Janey ; Rolando, Anna ; Sahly, Yousif ; Sidler, Kelley ; Widmer, W.Rick ; O'Keefe, Stephen J

Bioorganic & Medicinal Chemistry Letters, 1998, Vol.8(19), pp.2689-2694 [Peer Reviewed Journal]

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Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists

Doherty, George A ; Yang, Ginger X ; Borges, Edite ; Chang, Linda L ; Maccoss, Malcolm ; Tong, Sharon ; Kidambi, Usha ; Egger, Linda A ; Mccauley, Ermenegilda ; Van Riper, Gail ; Mumford, Richard A ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(11), pp.1501-1505 [Peer Reviewed Journal]

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20
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Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase

Durette, Philippe L ; Chabin, Renee M ; Fletcher, Daniel S ; Green, Barbara G ; Hanlon, William A ; Humes, John L ; Knight, Wilson B ; Lanza, Thomas J ; Mumford, Richard A ; Pacholok, Stephen ; Maccoss, Malcolm

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(3), pp.271-274 [Peer Reviewed Journal]

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21
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C-H Cyanation of 6-Ring N-Containing Heteroaromatics

Elbert, Bryony L ; Farley, Alistair J M ; Gorman, Timothy W ; Johnson, Tarn C ; Genicot, Christophe ; Lallemand, Bénédicte ; Pasau, Patrick ; Flasz, Jakub ; Castro, José L ; Maccoss, Malcolm ; Paton, Robert S ; Schofield, Christopher J ; Smith, Martin D ; Willis, Michael C ; Dixon, Darren J

Chemistry (Weinheim an der Bergstrasse, Germany), 20 October 2017, Vol.23(59), pp.14733-14737 [Peer Reviewed Journal]

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22
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Structure-activity relationship of purine ribonucleosides for inhibition of hepatitis C virus RNA-dependent RNA polymerase

Eldrup, Anne B ; Allerson, Charles R ; Bennett, C Frank ; Bera, Sanjib ; Bhat, Balkrishen ; Bhat, Neelima ; Bosserman, Michele R ; Brooks, Jennifer ; Burlein, Christine ; Carroll, Steven S ; Cook, P Dan ; Getty, Krista L ; Maccoss, Malcolm ; Mcmasters, Daniel R ; Olsen, David B ; Prakash, Thazha P ; Prhavc, Marija ; Song, Quanlai ; Tomassini, Joanne E ; Xia, Jie

Journal of medicinal chemistry, 22 April 2004, Vol.47(9), pp.2283-95 [Peer Reviewed Journal]

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Structure-activity relationship of heterobase-modified 2'-C-methyl ribonucleosides as inhibitors of hepatitis C virus RNA replication

Eldrup, Anne B ; Prhavc, Marija ; Brooks, Jennifer ; Bhat, Balkrishen ; Prakash, Thazha P ; Song, Quanlai ; Bera, Sanjib ; Bhat, Neelima ; Dande, Prasad ; Cook, P Dan ; Bennett, C Frank ; Carroll, Steven S ; Ball, Richard G ; Bosserman, Michele ; Burlein, Christine ; Colwell, Lawrence F ; Fay, John F ; Flores, Osvaldo A ; Getty, Krista ; Lafemina, Robert L ; Leone, Joseph ; Maccoss, Malcolm ; Mcmasters, Daniel R ; Tomassini, Joanne E ; Von Langen, Derek ; Wolanski, Bohdan ; Olsen, David B

Journal of medicinal chemistry, 07 October 2004, Vol.47(21), pp.5284-97 [Peer Reviewed Journal]

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Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides
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Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides

Esser, Craig K. ; Bugianesi, Robert L. ; Caldwell, Charles G. ; Chapman, Kevin T. ; Durette, Philippe L. ; Girotra, Narindar N. ; Kopka, Ihor E. ; Lanza, Thomas J. ; Levorse, Dorothy A. ; Maccoss, Malcolm ; Owens, Karen A. ; Ponpipom, Mitree M. ; Simeone, Joseph P. ; Harrison, Richard K. ; Niedzwiecki, Lisa ; Becker, Joseph W. ; Marcy, Alice I. ; Axel, Melinda G. ; Christen, Amy J. ; Mcdonnell, Joseph ; Moore, Vernon L. ; Olszewski, Julie M. ; Saphos, Cheryl ; Visco, Denise M. ; Shen, Frank ; Colletti, Adria ; Krieter, Philip A. ; Hagmann, William K.

Journal of Medicinal Chemistry, 03/1997, Vol.40(6), pp.1026-1040 [Peer Reviewed Journal]

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25
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Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR

Finke, Paul E ; Meurer, Laura C ; Levorse, Dorothy A ; Mills, Sander G ; Maccoss, Malcolm ; Sadowski, Sharon ; Cascieri, Margaret A ; Tsao, Kwei-Lan ; Chicchi, Gary G ; Metzger, Joseph M ; Macintyre, D. Euan

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4497-4503 [Peer Reviewed Journal]

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Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure–activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

Finke, Paul E ; Meurer, Laura C ; Oates, Bryan ; Mills, Sander G ; Maccoss, Malcolm ; Malkowitz, Lorraine ; Springer, Martin S ; Daugherty, Bruce L ; Gould, Sandra L ; Demartino, Julie A ; Siciliano, Salvatore J ; Carella, Anthony ; Carver, Gwen ; Holmes, Karen ; Danzeisen, Renee ; Hazuda, Daria ; Kessler, Joseph ; Lineberger, Janet ; Miller, Michael ; Schleif, William A ; Emini, Emilio A

Bioorganic & Medicinal Chemistry Letters, January 2001, Vol.11(2), pp.265-270 [Peer Reviewed Journal]

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Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure–Activity relationships for 1-[ N-(Methyl)- N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-( N-(alkyl)- N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes

Finke, Paul E ; Oates, Bryan ; Mills, Sander G ; Maccoss, Malcolm ; Malkowitz, Lorraine ; Springer, Martin S ; Gould, Sandra L ; Demartino, Julie A ; Carella, Anthony ; Carver, Gwen ; Holmes, Karen ; Danzeisen, Renee ; Hazuda, Daria ; Kessler, Joseph ; Lineberger, Janet ; Miller, Michael ; Schleif, William A ; Emini, Emilio A

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(18), pp.2475-2479 [Peer Reviewed Journal]

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Phosphoramidate prodrugs of 2'-C-methylcytidine for therapy of hepatitis C virus infection

Gardelli, Cristina ; Attenni, Barbara ; Donghi, Monica ; Meppen, Malte ; Pacini, Barbara ; Harper, Steven ; Di Marco, Annalise ; Fiore, Fabrizio ; Giuliano, Claudio ; Pucci, Vincenzo ; Laufer, Ralph ; Gennari, Nadia ; Marcucci, Isabella ; Leone, Joseph F ; Olsen, David B ; Maccoss, Malcolm ; Rowley, Michael ; Narjes, Frank

Journal of medicinal chemistry, 10 September 2009, Vol.52(17), pp.5394-407 [Peer Reviewed Journal]

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29
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Novel methods to functionalize thiazolo[4,5- c]pyridines

Girijavallabhan, Vinay ; Arasappan, Ashok ; Bennett, Frank ; Huang, Yuhua ; George Njoroge, F ; Maccoss, Malcolm

Tetrahedron Letters, 2010, Vol.51(21), pp.2797-2799 [Peer Reviewed Journal]

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Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors

Girijavallabhan, Vinay M ; Alvarez, Carmen ; Bennett, Frank ; Chen, Lei ; Gavalas, Stephen ; Huang, Yuhua ; Kim, Seong-Heon ; Kosinski, Aneta ; Pinto, Patrick ; Rizvi, Razia ; Rossman, Randall ; Shankar, Bandarpalle ; Tong, Ling ; Velazquez, Francisco ; Venkatraman, Srikanth ; Verma, Vishal A ; Kozlowski, Joseph ; Shih, Neng-Yang ; Piwinski, John J ; Maccoss, Malcolm ; Kwong, Cecil D ; Bansal, Namita ; Clark, Jeremy L ; Fowler, Anita T ; Kezar, Hollis S ; Valiyaveettil, Jacob ; Reynolds, Robert C ; Maddry, Joseph A ; Ananthan, Subramaniam ; Secrist, John A ; Li, Cheng ; Chase, Robert ; Curry, Stephanie ; Huang, Hsueh-Cheng ; Tong, Xiao ; Njoroge, F George ; Arasappan, Ashok

Bioorganic & medicinal chemistry letters, 01 September 2012, Vol.22(17), pp.5652-7 [Peer Reviewed Journal]

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31
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An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines

Guiadeen, Deodialsingh ; Kothandaraman, Shankaran ; Yang, Lihu ; Mills, Sander G ; Maccoss, Malcolm

Tetrahedron Letters, 2008, Vol.49(44), pp.6368-6370 [Peer Reviewed Journal]

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Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase

Guthikonda, Ravindra N ; Shah, Shrenik K ; Pacholok, Stephen G ; Humes, John L ; Mumford, Richard A ; Grant, Stephan K ; Chabin, Renee M ; Green, Barbara G ; Tsou, Nancy ; Ball, Richard ; Fletcher, Daniel S ; Luell, Silvi ; Euan Macintyre, D ; Maccoss, Malcolm

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(8), pp.1997-2001 [Peer Reviewed Journal]

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33
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Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

Hagmann, William K ; Caldwell, Charles G ; Chen, Ping ; Durette, Philippe L ; Esser, Craig K ; Lanza, Thomas J ; Kopka, Ihor E ; Guthikonda, Ravi ; Shah, Shrenik K ; Maccoss, Malcolm ; Chabin, Renee M ; Fletcher, Daniel ; Grant, Stephan K ; Green, Barbara G ; Humes, John L ; Kelly, Theresa M ; Luell, Sylvie ; Meurer, Roger ; Moore, Vernon ; Pacholok, Stephen G ; Pavia, Tony ; Williams, Hollis R ; Wong, Kenny K

Bioorganic & Medicinal Chemistry Letters, 2000, Vol.10(17), pp.1975-1978 [Peer Reviewed Journal]

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The discovery of sulfonylated dipeptides as Potent VLA-4 antagonists

Hagmann, William K ; Durette, Philippe L ; Lanza, Thomas ; Kevin, Nancy Jo ; de Laszlo, Stephen E ; Kopka, Ihor E ; Young, David ; Magriotis, Plato A ; Li, Bing ; Lin, Linus S ; Yang, Ginger ; Kamenecka, Theodore ; Chang, Linda L ; Wilson, Jonathan ; Maccoss, Malcolm ; Mills, Sander G ; Van Riper, Gail ; Mccauley, Ermengilda ; Egger, Linda A ; Kidambi, Usha ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Johannes ; Tong, Sharon ; Fenyk-Melody, Judy ; Owens, Karen ; Levorse, Dorothy ; Kim, Philip ; Schmidt, John A ; Mumford, Richard A

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(20), pp.2709-2713 [Peer Reviewed Journal]

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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent Anti-HIV activity

Hale, Jeffrey J ; Budhu, Richard J ; Holson, Edward B ; Finke, Paul E ; Oates, Bryan ; Mills, Sander G ; Maccoss, Malcolm ; Gould, Sandra L ; Demartino, Julie A ; Springer, Martin S ; Siciliano, Salvatore ; Malkowitz, Lorraine ; Schleif, William A ; Hazuda, Daria ; Miller, Michael ; Kessler, Joseph ; Danzeisen, Renee ; Holmes, Karen ; Lineberger, Janet ; Carella, Anthony ; Carver, Gwen ; Emini, Emilio

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(20), pp.2741-2745 [Peer Reviewed Journal]

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