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1
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Small molecule modulators of toll-like receptors

Czarniecki, Michael

Journal of medicinal chemistry, 13 November 2008, Vol.51(21), pp.6621-6 [Peer Reviewed Journal]

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An improved synthesis of 2-oxa-7-azaspiro[3,5]nonane and analogs as novel reagents in medicinal chemistry

Xu, Ruo ; Czarniecki, Michael ; Man, Jos de ; Pan, Jianping ; Qiang, Li ; Root, Yuriko ; Ying, Shihong ; Su, Jing ; Sun, Xijun ; Zhang, Yuping ; Yu, Tao ; Zhang, Yang ; Hu, Tao ; Chen, Shu-Hui

Tetrahedron Letters, 29 June 2011, Vol.52(26), pp.3266-3270 [Peer Reviewed Journal]

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Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors

Wang, Yu-Sen ; Strickland, Corey ; Voigt, Johannes H ; Kennedy, Matthew E ; Beyer, Brian M ; Senior, Mary M ; Smith, Elizabeth M ; Nechuta, Terry L ; Madison, Vincent S ; Czarniecki, Michael ; Mckittrick, Brian A ; Stamford, Andrew W ; Parker, Eric M ; Hunter, John C ; Greenlee, William J ; Wyss, Daniel F

Journal of medicinal chemistry, 11 February 2010, Vol.53(3), pp.942-50 [Peer Reviewed Journal]

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4
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An efficient synthesis of Wiedendiol-A from (+)-sclareolide

Chackalamannil, Samuel ; Wang, Yuguang ; Xia, Yan ; Czarniecki, Michael

Tetrahedron Letters, 1995, Vol.36(30), pp.5315-5318 [Peer Reviewed Journal]

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Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo

Sun, Zhong-Yue ; Asberom, Theodros ; Bara, Thomas ; Bennett, Chad ; Burnett, Duane ; Chu, Inhou ; Clader, John ; Cohen-Williams, Mary ; Cole, David ; Czarniecki, Michael ; Durkin, James ; Gallo, Gioconda ; Greenlee, William ; Josien, Hubert ; Huang, Xianhai ; Hyde, Lynn ; Jones, Nicholas ; Kazakevich, Irina ; Li, Hongmei ; Liu, Xiaoxiang ; Lee, Julie ; Maccoss, Malcolm ; Mandal, Mihir B ; Mccracken, Troy ; Nomeir, Amin ; Mazzola, Robert ; Palani, Anandan ; Parker, Eric M ; Pissarnitski, Dmitri A ; Qin, Jun ; Song, Lixin ; Terracina, Giuseppe ; Vicarel, Monica ; Voigt, Johannes ; Xu, Ruo ; Zhang, Lili ; Zhang, Qi ; Zhao, Zhiqiang ; Zhu, Xiaohong ; Zhu, Zhaoning

Journal of medicinal chemistry, 12 January 2012, Vol.55(1), pp.489-502 [Peer Reviewed Journal]

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Discovery of Cyclic Acylguanidines as Highly Potent and Selective β-Site Amyloid Cleaving Enzyme (BACE) Inhibitors: Part I–Inhibitor Design and Validation

Zhu, Zhaoning ; Sun, Zhong-Yue ; Ye, Yuanzan ; Voigt, Johannes ; Strickland, Corey ; Smith, Elizabeth M ; Cumming, Jared ; Wang, Lingyan ; Wong, Jesse ; Wang, Yu-Sen ; Wyss, Daniel F ; Chen, Xia ; Kuvelkar, Reshma ; Kennedy, Matthew E ; Favreau, Leonard ; Parker, Eric ; Mckittrick, Brian A ; Stamford, Andrew ; Czarniecki, Michael ; Greenlee, William ; Hunter, John C Argonne National Lab. (Anl), Argonne, Il (United States). Advanced Photon Source (APS) (Corporate Author)

Journal of Medicinal Chemistry, 20 November 2013, Vol.53((3) ; 02, 2010) [Peer Reviewed Journal]

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7
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Synthesis and SAR development of novel P2X 7 receptor antagonists for the treatment of pain: Part 2

Brumfield, Stephanie ; Matasi, Julius J ; Tulshian, Deen ; Czarniecki, Michael ; Greenlee, William ; Garlisi, Charles ; Qiu, Hongchen ; Devito, Kristine ; Chen, Shu-Cheng ; Sun, Yongliang ; Bertorelli, Rosalia ; Ansell, Justin ; Geiss, William ; Le, Van-Duc ; Martin, Gregory S ; Vellekoop, Samuel A ; Haber, James ; Allard, Melissa L

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(24), pp.7287-7290 [Peer Reviewed Journal]

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The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer’s disease

Li, Hongmei ; Qin, Jun ; Dhondi, Pawan ; Zhou, Wei ; Vicarel, Monica ; Bara, Thomas ; Cole, David ; Josien, Hubert ; Pissarnitski, Dmitri ; Zhu, Zhaoning ; Palani, Anandan ; Aslanian, Robert ; Clader, John ; Czarniecki, Michael ; Greenlee, William ; Cohen-Williams, Mary ; Hyde, Lynn ; Song, Lixin ; Zhang, Lili ; Chu, Inhou ; Huang, Xianhai

Bioorganic & Medicinal Chemistry Letters, 15 January 2013, Vol.23(2), pp.466-471 [Peer Reviewed Journal]

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9
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Guanine hydrolysis under basic conditions to substituted imidazoles

Gala, Dinesh ; Puar, Mohindar S ; Czarniecki, Michael ; Das, Pradip R ; Kugelman, Max ; Kaminski, James J

Tetrahedron Letters, 2000, Vol.41(26), pp.5025-5029 [Peer Reviewed Journal]

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10
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Dihydrodithioisocoumarin: Novel electrophilic reaction of carbon disulfide with phenethyl alcohol derivatives

Czarniecki, Michael ; Kluttz, Robert Q

Tetrahedron Letters, 1979, Vol.20(51), pp.4893-4894 [Peer Reviewed Journal]

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11
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Corrigendum to “Discovery and SAR of cyclic isothioureas as novel NPY Y 1 receptor antagonists” [Bioorg. Med. Chem. Lett. 19 (2009) 6801]

Sun, Zhong-Yue ; Zhu, Zhaoning ; Ye, Yuanzan ; Mckittrick, Brian ; Czarniecki, Michael ; Greenlee, William ; Mullins, Deborra ; Guzzi, Mario

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(5), pp.1800-1800 [Peer Reviewed Journal]

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12
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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Cumming, Jared N ; Smith, Elizabeth M ; Wang, Lingyan ; Misiaszek, Jeffrey ; Durkin, James ; Pan, Jianping ; Iserloh, Ulrich ; Wu, Yusheng ; Zhu, Zhaoning ; Strickland, Corey ; Voigt, Johannes ; Chen, Xia ; Kennedy, Matthew E ; Kuvelkar, Reshma ; Hyde, Lynn A ; Cox, Kathleen ; Favreau, Leonard ; Czarniecki, Michael F ; Greenlee, William J ; Mckittrick, Brian A ; Parker, Eric M ; Stamford, Andrew W

Bioorganic & Medicinal Chemistry Letters, 01 April 2012, Vol.22(7), pp.2444-2449 [Peer Reviewed Journal]

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13
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Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis

Su, Jing ; Mckittrick, Brian A ; Tang, Haiqun ; Czarniecki, Michael ; Greenlee, William J ; Hawes, Brian E ; O’neill, Kim

Bioorganic & Medicinal Chemistry, 2005, Vol.13(5), pp.1829-1836 [Peer Reviewed Journal]

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14
Synthesis of C3 Heteroatom-Substituted Azetidinones That Display Potent Cholesterol Absorption Inhibitory Activity
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Synthesis of C3 Heteroatom-Substituted Azetidinones That Display Potent Cholesterol Absorption Inhibitory Activity

Mckittrick, Brian A. ; Ma, Ke ; Huie, Keith ; Yumibe, Nathan ; Davis, Harry ; Clader, John W. ; Czarniecki, Michael ; Mcphail, Andrew T.

Journal of Medicinal Chemistry, 02/1998, Vol.41(5), pp.752-759 [Peer Reviewed Journal]

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15
Synthesis and Evaluation of Polycyclic Pyrazolo[3,4- d ]pyrimidines as PDE1 and PDE5 cGMP Phosphodiesterase Inhibitors
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Synthesis and Evaluation of Polycyclic Pyrazolo[3,4- d ]pyrimidines as PDE1 and PDE5 cGMP Phosphodiesterase Inhibitors

Xia, Yan ; Chackalamannil, Samuel ; Czarniecki, Michael ; Tsai, Hsingan ; Vaccaro, Henry ; Cleven, Renee ; Cook, John ; Fawzi, Ahmad ; Watkins, Robert ; Zhang, Hongtao

Journal of Medicinal Chemistry, 12/1997, Vol.40(26), pp.4372-4377 [Peer Reviewed Journal]

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16
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Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents

Chackalamannil, Samuel ; Xia, Yan ; Greenlee, William J ; Clasby, Martin ; Doller, Darìo ; Tsai, Hsingan ; Asberom, Theodros ; Czarniecki, Michael ; Ahn, Ho-Sam ; Boykow, George ; Foster, Carolyn ; Agans-Fantuzzi, Jacqueline ; Bryant, Matthew ; Lau, Janice ; Chintala, Madhu

Journal of medicinal chemistry, 22 September 2005, Vol.48(19), pp.5884-7 [Peer Reviewed Journal]

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17
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Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease

Huang, Xianhai ; Zhou, Wei ; Liu, Xiaoxiang ; Li, Hongmei ; Sun, George ; Mandal, Mihirbaran ; Vicarel, Monica ; Zhu, Xiaohong ; Bennett, Chad ; Mccraken, Troy ; Pissarnitski, Dmitri ; Zhao, Zhiqiang ; Cole, David ; Gallo, Gioconda ; Zhu, Zhaoning ; Palani, Anandan ; Aslanian, Robert ; Clader, John ; Czarniecki, Michael ; Greenlee, William ; Burnett, Duane ; Cohen-Williams, Mary ; Hyde, Lynn ; Song, Lixin ; Zhang, Lili ; Chu, Inhou ; Buevich, Alexei

ACS medicinal chemistry letters, 08 November 2012, Vol.3(11), pp.931-5 [Peer Reviewed Journal]

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18
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Iminopyrimidinones: A novel pharmacophore for the development of orally active renin inhibitors

Mckittrick, Brian A ; Caldwell, John P ; Bara, Thomas ; Boykow, George ; Chintala, Madhu ; Clader, John ; Czarniecki, Michael ; Courneya, Brandy ; Duffy, Ruth ; Fleming, Linda ; Giessert, Rachel ; Greenlee, William J ; Heap, Charles ; Hong, Liwu ; Huang, Ying ; Iserloh, Ulrich ; Josien, Hubert ; Khan, Tanweer ; Korfmacher, Walter ; Liang, Xian ; Mazzola, Robert ; Mitra, Soumya ; Moore, Kristina ; Orth, Peter ; Rajagopalan, Murali ; Roy, Sudipta ; Sakwa, Samuel ; Strickland, Corey ; Vaccaro, Henry ; Voigt, Johannes ; Wang, Hongwu ; Wong, Jesse ; Zhang, Rumin ; Zych, Andrew

Bioorganic & Medicinal Chemistry Letters, 01 April 2015, Vol.25(7), pp.1592-1596 [Peer Reviewed Journal]

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19
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T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones—optimization, design and synthesis

Smith, Elizabeth M ; Sorota, Steve ; Kim, Hyunjin M ; Mckittrick, Brian A ; Nechuta, Terry L ; Bennett, Chad ; Knutson, Chad ; Burnett, Duane A ; Kieselgof, Jane ; Tan, Zheng ; Rindgen, Diane ; Bridal, Terry ; Zhou, Xiaoping ; Jia, Yu-Ping ; Dong, Zoe ; Mullins, Debbie ; Zhang, Xiaoping ; Priestley, Tony ; Correll, Craig C ; Tulshian, Deen ; Czarniecki, Michael ; Greenlee, William J

Bioorganic & Medicinal Chemistry Letters, 01 August 2010, Vol.20(15), pp.4602-4606 [Peer Reviewed Journal]

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20
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Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening

Cavasotto, Claudio N ; Orry, Andrew J W ; Murgolo, Nicholas J ; Czarniecki, Michael F ; Kocsi, Sue Ann ; Hawes, Brian E ; O'Neill, Kim A ; Hine, Heather ; Burton, Marybeth S ; Voigt, Johannes H ; Abagyan, Ruben A ; Bayne, Marvin L ; Monsma, Frederick J

Journal of medicinal chemistry, 14 February 2008, Vol.51(3), pp.581-8 [Peer Reviewed Journal]

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21
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Metabolism-based identification of a potent thrombin receptor antagonist

Clasby, Martin C ; Chackalamannil, Samuel ; Czarniecki, Michael ; Doller, Dario ; Eagen, Keith ; Greenlee, William ; Kao, Grace ; Lin, Yan ; Tsai, Hsingan ; Xia, Yan ; Ahn, Ho-Sam ; Agans-Fantuzzi, Jacqueline ; Boykow, George ; Chintala, Madhu ; Foster, Carolyn ; Smith-Torhan, April ; Alton, Kevin ; Bryant, Matthew ; Hsieh, Yunsheng ; Lau, Janice ; Palamanda, Jairam

Journal of medicinal chemistry, 11 January 2007, Vol.50(1), pp.129-38 [Peer Reviewed Journal]

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22
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Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists

Zhu, Zhaoning ; Sun, Zhong-Yue ; Ye, Yuanzan ; Mckittrick, Brian ; Greenlee, William ; Czarniecki, Michael ; Fawzi, Ahmad ; Zhang, Hongtao ; Lachowicz, Jean E

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(17), pp.5218-5221 [Peer Reviewed Journal]

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23
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Discovery and SAR of cyclic isothioureas as novel NPY Y 1 receptor antagonists

Sun, Zhong-Yue ; Zhu, Zhaoning ; Ye, Yuanzan ; Mckittrick, Brian ; Czarniecki, Michael ; Greenlee, William ; Mullins, Deborra ; Guzzi, Mario

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(23), pp.6801-6805 [Peer Reviewed Journal]

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24
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The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAgg III conditions

Doller, Darío ; Chackalamannil, Samuel ; Stamford, Andrew ; Mckittrick, Brian ; Czarniecki, Michael

Bioorganic & Medicinal Chemistry Letters, 1997, Vol.7(11), pp.1381-1386 [Peer Reviewed Journal]

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25
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Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists

Doller, Darío ; Chackalamannil, Samuel ; Czarniecki, Michael ; Mcquade, Robert ; Ruperto, Vilma

Bioorganic & Medicinal Chemistry Letters, 1999, Vol.9(6), pp.901-906 [Peer Reviewed Journal]

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26
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Potent, low molecular weight thrombin receptor antagonists

Chackalamannil, Samuel ; Doller, Darı́o ; Eagen, Keith ; Czarniecki, Michael ; Ahn, Ho-Sam ; Foster, Carolyn J ; Boykow, George

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(21), pp.2851-2853 [Peer Reviewed Journal]

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27
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Synthesis and structure–activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists

Lai, Gaifa ; Merritt, J. Robert ; He, Zhenmin ; Feng, Daming ; Chao, Jianhua ; Czarniecki, Michael F ; Rokosz, Laura L ; Stauffer, Tara M ; Rindgen, Diane ; Taveras, Arthur G

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(6), pp.1864-1868 [Peer Reviewed Journal]

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28
Potent Tetracyclic Guanine Inhibitors of PDE1 and PDE5 Cyclic Guanosine Monophosphate Phosphodiesterases with Oral Antihypertensive Activity
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Potent Tetracyclic Guanine Inhibitors of PDE1 and PDE5 Cyclic Guanosine Monophosphate Phosphodiesterases with Oral Antihypertensive Activity

Ahn, Ho-Sam ; Bercovici, Ana ; Boykow, George ; Bronnenkant, Alan ; Chackalamannil, Samuel ; Chow, Jason ; Cleven, Renee ; Cook, John ; Czarniecki, Michael ; Domalski, Carol ; Fawzi, Ahmad ; Green, Michael ; Gündes, Asli ; Ho, Ginny ; Laudicina, Malvina ; Lindo, Neil ; Ma, Ke ; Manna, Mahua ; Mckittrick, Brian ; Mirzai, Bita ; Nechuta, Terry ; Neustadt, Bernard ; Puchalski, Chester ; Pula, Kathryn ; Silverman, Lisa ; Smith, Elizabeth ; Stamford, Andrew ; Tedesco, Richard P. ; Tsai, Hsingan ; Tulshian, Deen ; Vaccaro, Henry ; Watkins, Robert W. ; Weng, Xiaoyu ; Witkowski, Joseph T. ; Xia, Yan ; Zhang, Hongtao

Journal of Medicinal Chemistry, 07/1997, Vol.40(14), pp.2196-2210 [Peer Reviewed Journal]

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29
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Novel inhibitors of cholesteryl ester transfer protein

Chackalamannil, Samuel ; Xia, Yan ; Wang, Yuguang ; Tsai, Hsingan ; Czarniecki, Michael ; Wang, Suke ; Clemmons, Anthony ; Ahn, Ho-Sam ; Boykow, George

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(17), pp.2005-2010 [Peer Reviewed Journal]

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30
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Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11

Mckittrick, Brian A ; Stamford, Andrew W ; Xiaoyu Weng ; Ke Ma ; Chackalamannil, Samuel ; Czarniecki, Michael ; Cleven, Reneém ; Fawzi, Ahmad B

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(14), pp.1629-1634 [Peer Reviewed Journal]

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31
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Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors

Mckittrick, Brian A ; Ma, Ke ; Dugar, Sundeep ; Clader, John W ; Davis, Harry ; Czarniecki, Michael ; Mcphail, Andrew T

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(16), pp.1947-1950 [Peer Reviewed Journal]

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32
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Substituted 1,3,5-triazines as cholesteryl ester transfer protein inhibitors

Yan Xia ; Mirzai, Bita ; Chackalamannil, Samuel ; Czarniecki, Michael ; Wang, Suke ; Clemmons, Anthony ; Ahn, Ho-Sam ; Boykow, George C

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(7), pp.919-922 [Peer Reviewed Journal]

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33
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Highly potent and selective inhibitors of endothelin converting enzyme

Chackalamannil, Samuel ; Chung, Shin ; Stamford, Andrew W ; Mckittrick, Brian A ; Wang, Yuguang ; Tsai, Hsingan ; Cleven, Reneé ; Fawzi, Ahmad ; Czarniecki, Michael

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(11), pp.1257-1260 [Peer Reviewed Journal]

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34
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Himbacine derived thrombin receptor (PAR-1) antagonists: Structure–activity relationship of the lactone ring

Xia, Yan ; Chackalamannil, Samuel ; Chan, Tze-Ming ; Czarniecki, Michael ; Doller, Darío ; Eagen, Keith ; Greenlee, William J ; Tsai, Hsingan ; Wang, Yuguang ; Ahn, Ho-Sam ; Boykow, George C ; Mcphail, Andrew T

Bioorganic & Medicinal Chemistry Letters, 15 September 2006, Vol.16(18), pp.4969-4972 [Peer Reviewed Journal]

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35
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Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Ahn, Ho-Sam ; Arik, Leyla ; Boykow, George ; Burnett, Duane A ; Caplen, Mary Ann ; Czarniecki, Michael ; Domalski, Martin S ; Foster, Carolyn ; Manna, Mahua ; Stamford, Andrew W ; Wu, Yusheng

Bioorganic & Medicinal Chemistry Letters, 1999, Vol.9(14), pp.2073-2078 [Peer Reviewed Journal]

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36
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