Search Results - "Rajapakse, Hemaka A."

Asymmetric Syntheses of Pectenotoxins-4 and -8, Part II: Synthesis of the C20-C30 and C31-C40 Subunits and Fragment Assembly by Evans, David A., Rajapakse, Hemaka A., Chiu, Anna, Stenkamp, Dirk

“…The total syntheses of the marine macrolides pectenotoxins‐4 and ‐8 have been realized. The pectenotoxins are a new class of marine macrolides that exhibit a…”
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Asymmetric Syntheses of Pectenotoxins-4 and -8, Part I: Synthesis of the C1-C19 Subunit by Evans, David A., Rajapakse, Hemaka A., Stenkamp, Dirk

“…The total syntheses of the marine macrolides pectenotoxins‐4 and ‐8 have been realized. The pectenotoxins are a new class of marine macrolides that exhibit a…”
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Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors by Lindsley, Stacey R., Moore, Keith P., Rajapakse, Hemaka A., Selnick, Harold G., Young, Mary Beth, Zhu, Hong, Munshi, Sanjeev, Kuo, Lawrence, McGaughey, Georgia B., Colussi, Dennis, Crouthamel, Ming-Chih, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Seabrook, Guy R., Hazuda, Daria J., Pudvah, Nicole T., Hochman, Jerome H., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.

“…This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors,…”
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Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors by Zhu, Hong, Young, Mary B., Nantermet, Philippe G., Graham, Samuel L., Colussi, Dennis, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Shi, Xiao-ping, Tugusheva, Katherine, Holahan, Marie A., Michener, Maria S., Cook, Jacquelynn J., Simon, Adam, Hazuda, Daria J., Vacca, Joseph P., Rajapakse, Hemaka A.

“…This Letter describes the one pot synthesis of tertiary carbinamine 3 and related analogs of brain penetrant BACE-1 inhibitors via the alkylation of the Schiff…”
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Structure-Based Design of Potent and Selective Cell-Permeable Inhibitors of Human β-Secretase (BACE-1) by Stachel, Shawn J, Coburn, Craig A, Steele, Thomas G, Jones, Kristen G, Loutzenhiser, Elizabeth F, Gregro, Alison R, Rajapakse, Hemaka A, Lai, Ming-Tain, Crouthamel, Ming-Chih, Xu, Min, Tugusheva, Katherine, Lineberger, Janet E, Pietrak, Beth L, Espeseth, Amy S, Shi, Xiao-Ping, Chen-Dodson, Elizabeth, Holloway, M. Katharine, Munshi, Sanjeev, Simon, Adam J, Kuo, Lawrence, Vacca, Joseph P

“…We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an…”
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Potent, selective and orally bioavailable leucine-rich repeat kinase 2 (LRRK2) inhibitors by Greshock, Thomas J., Sanders, John M., Drolet, Robert E., Rajapakse, Hemaka A., Chang, Ronald K., Kim, Boyoung, Rada, Vanessa L., Tiscia, Heather E., Su, Hua, Lai, Ming-Tain, Sur, Sylvie M., Sanchez, Rosa I., Bilodeau, Mark T., Renger, John J., Kern, Jonathan T., McCauley, John A.

“…[Display omitted] Familial Parkinson’s disease cases have recently been associated with the leucine rich repeat kinase 2 (LRRK2) gene. It has been hypothesized…”
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Small molecule inhibitors of the XIAP protein-protein interaction by Rajapakse, Hemaka A

“…The X-linked inhibitor of apoptosis proteins (XIAP) is thought to play a key role in the unchecked proliferation of cancer cells by interfering with the…”
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Discovery of Oxadiazoyl Tertiary Carbinamine Inhibitors of β-Secretase (BACE-1) by Rajapakse, Hemaka A, Nantermet, Philippe G, Selnick, Harold G, Munshi, Sanjeev, McGaughey, Georgia B, Lindsley, Stacey R, Young, Mary Beth, Lai, Ming-Tain, Espeseth, Amy S, Shi, Xiao-Ping, Colussi, Dennis, Pietrak, Beth, Crouthamel, Ming-Chih, Tugusheva, Katherine, Huang, Qian, Xu, Min, Simon, Adam J, Kuo, Lawrence, Hazuda, Daria J, Graham, Samuel, Vacca, Joseph P

“…We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme β-secretase (BACE-1). These novel…”
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Attenuation of scratch‐induced reactive astrogliosis by novel EphA4 kinase inhibitors by Parmentier‐Batteur, Sophie, Finger, Eleftheria N., Krishnan, Raghu, Rajapakse, Hemaka A., Sanders, John M., Kandpal, Geeta, Zhu, Hong, Moore, Keith P., Regan, Christopher P., Sharma, Sujata, Hess, J. Fred, Williams, Theresa M., Reynolds, Ian J., Vacca, Joseph P., Mark, Robert J., Nantermet, Philippe G.

“…J. Neurochem. (2011) 118, 1016–1031. The EphA4 receptor and its ephrin ligands are involved in astrocytic gliosis following CNS injury. Therefore, a strategy…”
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Synthesis of Elenic Acid, an Inhibitor of Topoisomerase II by Hoye, Rebecca C, Baigorria, Alejandro S, Danielson, Michael E, Pragman, Alexa A, Rajapakse, Hemaka A

“…A short, efficient synthesis of elenic acid, a marine natural product with interesting biological activity, has been completed. Critical features of the…”
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Enantioselective total synthesis of altohyrtin C (spongistatin 2) by Evans, David A., Trotter, B.Wesley, Coleman, Paul J., Côté, Bernard, Dias, Luiz Carlos, Rajapakse, Hemaka A., Tyler, Andrew N.

“…The first total synthesis of a spongipyran macrolide, altohyrtin C, is described. The convergent synthesis strategy relies on a regioselective…”
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SAR of tertiary carbinamine derived BACE1 inhibitors: Role of aspartate ligand amine pKa in enzyme inhibition by RAJAPAKSE, Hemaka A, NANTERMET, Philippe G, LAI, Ming-Tain, ESPESETH, Amy S, SHI, Xiao-Ping, COLUSSI, Dennis, PIETRAK, Beth, CROUTHAMEL, Ming-Chih, TUGUSHEVA, Katherine, QIAN HUANG, MIN XU, SIMON, Adam J, SELNICK, Harold G, KUO, Lawrence, HAZUDA, Daria J, GRAHAM, Samuel, VACCA, Joseph P, BARROW, James C, MCGAUGHEY, Georgia B, MUNSHI, Sanjeev, LINDSLEY, Stacey R, YOUNG, Mary Beth, NGO, Phung L, KATHERINE HOLLOWAY, M

“…The optimization of tertiary carbinamine derived inhibitors of BACE1 from its discovery as an unstable lead to low nanomolar cell active compounds is…”
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β-Secretase (BACE-1) inhibitors: Accounting for 10s loop flexibility using rigid active sites by McGaughey, Georgia B., Colussi, Dennis, Graham, Samuel L., Lai, Ming-Tain, Munshi, Sanjeev K., Nantermet, Philippe G., Pietrak, Beth, Rajapakse, Hemaka A., Selnick, Harold G., Stauffer, Shaun R., Holloway, M. Katharine

“…BACE-1 crystal structures demonstrating 10s loop motion were used to correlate K i values from a series of tertiary carbinamine inhibitors with an empirical…”
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Strategies towards Improving the Pharmacokinetic Profile of ε-Substituted Lysinol-Derived HIV Protease Inhibitors by Rajapakse, Hemaka A., Walji, Abbas M., Moore, Keith P., Zhu, Hong, Mitra, Aurpon W., Gregro, Alison R., Tinney, Elizabeth, Burlein, Christine, Touch, Sinoeun, Paton, Brenda L., Carroll, Steven S., DiStefano, Daniel J., Lai, Ming-Tain, Grobler, Jay A., Sanchez, Rosa I., Williams, Theresa M., Vacca, Joseph P., Nantermet, Philippe G.

“…Compounds that are all HAART: Subsequent to accessing the S2 subpocket of HIV protease from the novel lysinol series of HIV protease inhibitors, we now report…”
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Evolution of Tertiary Carbinamine BACE‐1 Inhibitors: Aβ Reduction in Rhesus CSF upon Oral Dosing by Nantermet, Philippe G., Rajapakse, Hemaka A., Stanton, Mathew G., Stauffer, Shaun R., Barrow, James C., Gregro, Allison R., Moore, Keith P., Steinbeiser, Melissa A., Swestock, John, Selnick, Harold G., Graham, Samuel L., McGaughey, Georgia B., Colussi, Dennis, Lai, Ming‐Tain, Sankaranarayanan, Sethu, Simon, Adam J., Munshi, Sanjeev, Cook, Jacquelynn J., Holahan, Marie A., Michener, Maria S., Vacca, Joseph P.

“…Turning up the BACE: Incorporation of an isonicotinic core into oxadiazolyl tertiary carbinamine‐based inhibitors of BACE‐1 has led to the identification of an…”
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Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors by Moore, Keith P., Zhu, Hong, Rajapakse, Hemaka A., McGaughey, Georgia B., Colussi, Dennis, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Pudvah, Nicole T., Hochman, Jerome H., Allison, Timothy, Munshi, Sanjeev K., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.

“…This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues…”
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A mild and efficient one pot synthesis of 1,3,4-oxadiazoles from carboxylic acids and acyl hydrazides by Rajapakse, Hemaka A., Zhu, Hong, Young, Mary Beth, Mott, Bryan T.

“…A convenient one pot method for the synthesis of 2,5-disubstituted 1,3,4-oxadiazoles from carboxylic acids and acyl hydrazides is reported. Acid activation…”
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SAR of tertiary carbinamine derived BACE1 inhibitors: Role of aspartate ligand amine pK sub(a) in enzyme inhibition by Rajapakse, Hemaka A, Nantermet, Philippe G, Selnick, Harold G, Barrow, James C, McGaughey, Georgia B, Munshi, Sanjeev, Lindsley, Stacey R, Young, Mary Beth, Ngo, Phung L, Holloway, MKatherine, Lai, Ming-Tain, Espeseth, Amy S, Shi, Xiao-Ping, Colussi, Dennis, Pietrak, Beth, Crouthamel, Ming-Chih, Tugusheva, Katherine, Huang, Qian, Xu, Min, Simon, Adam J, Kuo, Lawrence, Hazuda, Daria J, Graham, Samuel, Vacca, Joseph P

“…The optimization of tertiary carbinamine derived inhibitors of BACE1 from its discovery as an unstable lead to low nanomolar cell active compounds is…”
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SAR of tertiary carbinamine derived BACE1 inhibitors: Role of aspartate ligand amine p K a in enzyme inhibition by Rajapakse, Hemaka A., Nantermet, Philippe G., Selnick, Harold G., Barrow, James C., McGaughey, Georgia B., Munshi, Sanjeev, Lindsley, Stacey R., Young, Mary Beth, Ngo, Phung L., Katherine Holloway, M., Lai, Ming-Tain, Espeseth, Amy S., Shi, Xiao-Ping, Colussi, Dennis, Pietrak, Beth, Crouthamel, Ming-Chih, Tugusheva, Katherine, Huang, Qian, Xu, Min, Simon, Adam J., Kuo, Lawrence, Hazuda, Daria J., Graham, Samuel, Vacca, Joseph P.

“…This Letter describes SAR of the tertiary carbinamine derived inhibitors of BACE1 revealed during the optimization of the unstable lead toward potent and…”
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Asymmetric synthesis of dihydroquinazolinones via directed ortho metalation and addition to tert-butanesulfinyl imines by Rajapakse, Hemaka A., Young, Mary Beth, Zhu, Hong, Charlton, Samantha, Tsou, Nancy N.

“…An asymmetric route to dihydroquinazolinones via the addition of ortho metalated substrates to tert-butanesulfinyl imines is reported. An asymmetric route to…”
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