Search Results - "CALDWELL, John P"

Protecting group free radical C-H trifluoromethylation of peptides by Ichiishi, Naoko, Caldwell, John P, Lin, Melissa, Zhong, Wendy, Zhu, Xiaohong, Streckfuss, Eric, Kim, Hai-Young, Parish, Craig A, Krska, Shane W

“…Two radical-based approaches have been developed to effect the trifluoromethylation of aryl C-H bonds in native peptides either using stoichiometric oxidant or…”
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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation by Mandal, Mihirbaran, Zhu, Zhaoning, Cumming, Jared N, Liu, Xiaoxiang, Strickland, Corey, Mazzola, Robert D, Caldwell, John P, Leach, Prescott, Grzelak, Michael, Hyde, Lynn, Zhang, Qi, Terracina, Giuseppe, Zhang, Lili, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Cox, Kathleen, Orth, Peter, Buevich, Alexei, Voigt, Johannes, Wang, Hongwu, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Parker, Eric M, Stamford, Andrew W

“…On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1–S3…”
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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9 by Petrilli, Whitney L, Adam, Gregory C, Erdmann, Roman S, Abeywickrema, Pravien, Agnani, Vijayalakshmi, Ai, Xi, Baysarowich, Jen, Byrne, Noel, Caldwell, John P, Chang, Wonsuk, DiNunzio, Edward, Feng, Zhe, Ford, Rachael, Ha, Sookhee, Huang, Yongcheng, Hubbard, Brian, Johnston, Jennifer M, Kavana, Michael, Lisnock, Jean-Marie, Liang, Rui, Lu, Jun, Lu, Zhijian, Meng, Juncai, Orth, Peter, Palyha, Oksana, Parthasarathy, Gopal, Salowe, Scott P, Sharma, Sujata, Shipman, Jennifer, Soisson, Stephen M, Strack, Alison M, Youm, Hyewon, Zhao, Kake, Zink, Deborah L, Zokian, Hratch, Addona, George H, Akinsanya, Karen, Tata, James R, Xiong, Yusheng, Imbriglio, Jason E

“…Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein…”
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Generation of Leads for γ‑Secretase Modulation by Mandal, Mihirbaran, Buevich, Alexei, Caldwell, John P, Hyde, Lynn, Huang, Xianhai, Liu, Xiaoxiang, McKittrick, Brian, Mazzola, Robert D, Pissarnitski, Dmitri, Palani, Anandan, Zhang, Lili, Parker, Eric, Xiao, Li, Rindgen, Diane, Zhu, Zhaoning

“…Herein, we disclose three structurally differentiated γ-secretase modulators (GSMs) based on an oxadiazine scaffold. The analogues from series I potently…”
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The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety by Ho, Ginny D., Anthes, John, Bercovici, Ana, Caldwell, John P., Cheng, Kuo-Chi, Cui, Xiaoming, Fawzi, Ahmad, Fernandez, Xiomara, Greenlee, William J., Hey, John, Korfmacher, Walter, Lu, Sherry X., McLeod, Robbie L., Ng, Fay, Torhan, April Smith, Tan, Zheng, Tulshian, Deen, Varty, Geoffrey B., Xu, Xiaoying, Zhang, Hongtao

“…The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1]octane)…”
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Evolving Epidemiology of Japanese Encephalitis: Implications for Vaccination by Caldwell, John P., Chen, Lin H., Hamer, Davidson H.

“…Purpose of Review We examine the present global burden of Japanese encephalitis (JE) in endemic populations, summarize published cases in travelers since 2009,…”
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Unprecedented Reversal of Regioselectivity during Methanolysis and an Interception of Curtius Rearrangement by Mandal, Mihirbaran, Buevich, Alexei V., Wang, Hongwu, Brunskill, Andrew, Orth, Peter, Caldwell, John P., Liu, Xiaoxiang, Mazzola, Robert, Cumming, Jared, McKittrick, Brian, Zhu, Zhaoning, Stamford, Andrew

“…Unprecedented reversal in regioselectivity during methanolysis of anhydrides due to the change in substitution pattern of fluorine in the phenyl moiety, and…”
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Cyp1 Inhibition Prevents Doxorubicin‐Induced Cardiomyopathy in a Zebrafish Heart‐Failure Model by Lam, Pui‐Ying, Kutchukian, Peter, Anand, Rajan, Imbriglio, Jason, Andrews, Christine, Padilla, Hugo, Vohra, Anita, Lane, Sarah, Parker, Dann L., Cornella Taracido, Ivan, Johns, Douglas G., Beerens, Manu, MacRae, Calum A., Caldwell, John P., Sorota, Steve, Asnani, Aarti, Peterson, Randall T.

“…Doxorubicin is a highly effective chemotherapy agent used to treat many common malignancies. However, its use is limited by cardiotoxicity, and cumulative…”
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Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands by Caldwell, John P., Matasi, Julius J., Zhang, Hongtao, Fawzi, Ahmad, Tulshian, Deen B.

“…A series of N-substituted analogs based upon the spiropiperidine core of 1 was synthesized and exhibited high binding affinity to the nociceptin (NOP)…”
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates by Mandal, Mihirbaran, Wu, Yusheng, Misiaszek, Jeffrey, Li, Guoqing, Buevich, Alexei, Caldwell, John P, Liu, Xiaoxiang, Mazzola, Robert D, Orth, Peter, Strickland, Corey, Voigt, Johannes, Wang, Hongwu, Zhu, Zhaoning, Chen, Xia, Grzelak, Michael, Hyde, Lynn A, Kuvelkar, Reshma, Leach, Prescott T, Terracina, Giuseppe, Zhang, Lili, Zhang, Qi, Michener, Maria S, Smith, Brad, Cox, Kathleen, Grotz, Diane, Favreau, Leonard, Mitra, Kaushik, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Kennedy, Matthew E, Parker, Eric M, Cumming, Jared N, Stamford, Andrew W

“…We describe successful efforts to optimize the in vivo profile and address off-target liabilities of a series of BACE1 inhibitors represented by 6 that…”
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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety by Mandal, Mihirbaran, Mitra, Kaushik, Grotz, Diane, Lin, Xinjie, Palamanda, Jairam, Kumari, Pramila, Buevich, Alexei, Caldwell, John P, Chen, Xia, Cox, Kathleen, Favreau, Leonard, Hyde, Lynn, Kennedy, Matthew E, Kuvelkar, Reshma, Liu, Xiaoxiang, Mazzola, Robert D, Parker, Eric, Rindgen, Diane, Sherer, Edward, Wang, Hongwu, Zhu, Zhaoning, Stamford, Andrew W, Cumming, Jared N

“…Herein we describe structure–activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent…”
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Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor by Mandal, Mihirbaran, Tan, Zheng, Madsen-Duggan, Christina, Buevich, Alexei V, Caldwell, John P, Dejesus, Reynalda, Flattery, Amy, Garlisi, Charles G, Gill, Charles, Ha, Sookhee Nicole, Ho, Ginny, Koseoglu, Sandra, Labroli, Marc, Basu, Kallol, Lee, Sang Ho, Liang, Lianzhu, Liu, Jenny, Mayhood, Todd, McGuinness, Debra, McLaren, David G, Wen, Xiujuan, Parmee, Emma, Rindgen, Diane, Roemer, Terry, Sheth, Payal, Tawa, Paul, Tata, James, Yang, Christine, Yang, Shu-Wei, Xiao, Li, Wang, Hao, Tan, Christopher, Tang, Haifeng, Walsh, Paul, Walsh, Erika, Wu, Jin, Su, Jing

“…We describe our optimization efforts to improve the physicochemical properties, solubility, and off-target profile of 1, an inhibitor of TarO, an early stage…”
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Discovery of potent wall teichoic acid early stage inhibitors by Labroli, Marc A., Caldwell, John P., Yang, Christine, Lee, Sang Ho, Wang, Hao, Koseoglu, Sandra, Mann, Paul, Yang, Shu-Wei, Xiao, Jing, Garlisi, Charles G., Tan, Christopher, Roemer, Terry, Su, Jing

“…Herein we describe the optimization of a series of inhibitors termed tarocins which demonstrate by genetic and biochemical means inhibition of TarO, the first…”
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Discovery of potent iminoheterocycle BACE1 inhibitors by Caldwell, John P., Mazzola, Robert D., Durkin, James, Chen, Joseph, Chen, Xia, Favreau, Leonard, Kennedy, Matthew, Kuvelkar, Reshma, Lee, Julie, McHugh, Nansie, McKittrick, Brian, Orth, Peter, Stamford, Andrew, Strickland, Corey, Voigt, Johannes, Wang, Liyang, Zhang, Lili, Zhang, Qi, Zhu, Zhaoning

“…The synthesis of a series of iminoheterocycles and their structure–activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed…”
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Iminopyrimidinones: A novel pharmacophore for the development of orally active renin inhibitors by 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

“…The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of…”
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Iminoheterocycles as γ-secretase modulators by Caldwell, John P., Bennett, Chad E., McCracken, Troy M., Mazzola, Robert D., Bara, Thomas, Buevich, Alexei, Burnett, Duane A., Chu, Inhou, Cohen-Williams, Mary, Josein, Hubert, Hyde, Lynn, Lee, Julie, McKittrick, Brian, Song, Lixin, Terracina, Giuseppe, Voigt, Johannes, Zhang, Lili, Zhu, Zhaoning

“…The synthesis of a novel series of iminoheterocycles and their structure–activity relationship (SAR) as modulators of γ-secretase activity will be detailed…”
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The discovery and synthesis of novel adenosine receptor (A 2A) antagonists by Matasi, Julius J., Caldwell, John P., Hao, Jinsong, Neustadt, Bernard, Arik, Leyla, Foster, Carolyn J., Lachowicz, Jean, Tulshian, Deen B.

“…The structure–activity relationship investigation using 1 as a template led to the identification of a novel class of compounds as potent and selective…”
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Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 2 by Caldwell, John P., Matasi, Julius J., Fernandez, Xiomara, McLeod, Robbie L., Zhang, Hongtao, Fawzi, Ahmad, Tulshian, Deen B.

“…A series of N-8 substituted analogs based upon the spiropiperidine core of the original lead compound 1 was synthesized. This lead has been elaborated to…”
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2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1 by Matasi, Julius J, Caldwell, John P, Zhang, Hongtao, Fawzi, Ahmad, Cohen-Williams, Mary E, Varty, Geoffrey B, Tulshian, Deen B

“…The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its…”
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3H-[1,2,4] -Triazolo[5,1-i]purin -5 -amine derivatives as adenosine A2A antagonists by SILVERMAN, Lisa S, CALDWELL, John P, ONGINI, Ennio, GREENLEE, William J, KISELGOF, Eugenia, MATASI, Julius J, TULSHIAN, Deen B, ARIK, Leyla, FOSTER, Carolyn, BERTORELLI, Rosalia, MONOPOLI, Angela

“…A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine…”
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