Search Results - "Lera Ruiz, Manuel de"

Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle by Favuzza, Paola, de Lera Ruiz, Manuel, Thompson, Jennifer K., Triglia, Tony, Ngo, Anna, Steel, Ryan W.J., Vavrek, Marissa, Christensen, Janni, Healer, Julie, Boyce, Christopher, Guo, Zhuyan, Hu, Mengwei, Khan, Tanweer, Murgolo, Nicholas, Zhao, Lianyun, Penington, Jocelyn Sietsma, Reaksudsan, Kitsanapong, Jarman, Kate, Dietrich, Melanie H., Richardson, Lachlan, Guo, Kai-Yuan, Lopaticki, Sash, Tham, Wai-Hong, Rottmann, Matthias, Papenfuss, Tony, Robbins, Jonathan A., Boddey, Justin A., Sleebs, Brad E., Sabroux, Hélène Jousset, McCauley, John A., Olsen, David B., Cowman, Alan F.

“…Artemisin combination therapy (ACT) is the main treatment option for malaria, which is caused by the intracellular parasite Plasmodium. However, increased…”
Get full text

Histamine H3 Receptor as a Drug Discovery Target by Berlin, Michael, Boyce, Christopher W, de Lera Ruiz, Manuel

Get full text

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications by de Lera Ruiz, Manuel, Kraus, Richard L

“…The tremendous therapeutic potential of voltage-gated sodium channels (Navs) has been the subject of many studies in the past and is of intense interest today…”
Get full text

Discovery of MK-8970: An Acetal Carbonate Prodrug of Raltegravir with Enhanced Colonic Absorption by Walji, Abbas M., Sanchez, Rosa I., Clas, Sophie-Dorothee, Nofsinger, Rebecca, de Lera Ruiz, Manuel, Li, Jing, Bennet, Amrithraj, John, Christopher, Bennett, David Jonathan, Sanders, John M., Di Marco, Christina N., Kim, Somang Hope, Balsells, Jaume, Ceglia, Scott S., Dang, Qun, Manser, Kimberly, Nissley, Becky, Wai, John S., Hafey, Michael, Wang, Junying, Chessen, Gene, Templeton, Allen, Higgins, John, Smith, Ronald, Wu, Yunhui, Grobler, Jay, Coleman, Paul J.

“…Developing new antiretroviral therapies for HIV‐1 infection with potential for less frequent dosing represents an important goal within drug discovery. Herein,…”
Get full text

Histamine H 3 Receptor as a Drug Discovery Target by Berlin, Michael, Boyce, Christopher W., de Lera Ruiz, Manuel

Get full text

Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax by Hodder, Anthony N, Christensen, Janni, Scally, Stephen, Triglia, Tony, Ngo, Anna, Birkinshaw, Richard W, Bailey, Brodie, Favuzza, Paola, Dietrich, Melanie H, Tham, Wai-Hong, Czabotar, Peter E, Lowes, Kym, Guo, Zhuyan, Murgolo, Nicholas, Lera Ruiz, Manuel de, McCauley, John A, Sleebs, Brad E, Olsen, David, Cowman, Alan F

“…Plasmepsins IX (PMIX) and X (PMX) are essential aspartyl proteases for Plasmodium spp. egress, invasion, and development. WM4 and WM382 inhibit PMIX and PMX in…”
Get full text

Synthesis of a CGRP Receptor Antagonist via an Asymmetric Synthesis of 3‑Fluoro-4-aminopiperidine by Molinaro, Carmela, Phillips, Eric M, Xiang, Bangping, Milczek, Erika, Shevlin, Michael, Balsells, Jaume, Ceglia, Scott, Chen, Jiahui, Chen, Lu, Chen, Qinghao, Fei, Zhongbo, Hoerrner, Scott, Qi, Ji, de Lera Ruiz, Manuel, Tan, Lushi, Wan, Baoqiang, Yin, Jingjun

“…A practical and efficient enantioselective synthesis of the calcitonin gene-related peptide receptor antagonist 1 has been developed. The key structural…”
Get full text

The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria by de Lera Ruiz, Manuel, Favuzza, Paola, Guo, Zhuyan, Zhao, Lianyun, Hu, Bin, Lei, Zhiyu, Zhan, Dongmei, Murgolo, Nicholas, Boyce, Christopher W., Vavrek, Marissa, Thompson, Jennifer, Ngo, Anna, Jarman, Kate E., Robbins, Johnathan, Boddey, Justin, Sleebs, Brad E., Lowes, Kym N., Cowman, Alan F., Olsen, David B., McCauley, John A.

“…Drug resistance to first-line antimalarialsincluding artemisininis increasing, resulting in a critical need for the discovery of new agents with novel…”
Get full text

Careful Navigation of the Crystallographic Landscape of MK-8970: A Racemic Acetal Carbonate Prodrug of Raltegravir by Tsou, Nancy, Shultz, C. Scott, Andreani, Teresa, Ball, Richard G, Brunskill, Andrew, Balsells, Jaume, Cohen, Ryan D, DaSilva, Jimmy, Li, Jing, Reamer, Robert A, de Lera Ruiz, Manuel, Variankaval, Narayan, Varsolona, Richard J, Yasuda, Nobuyoshi, York, Gregory

“…MK-8970 is an acetal carbonate prodrug of raltegravir (Isentress). This work presents the Merck team’s investigations into the polymorphism of MK-8970, the…”
Get full text

Stereoselective synthesis of highly functionalised P-stereogenic nucleosides via palladium-catalysed P–C cross-coupling reactions by Whittaker, Benjamin, Ruiz, Manuel de Lera, Hayes, Christopher J.

“…We have shown that the configuration at the P-stereogenic centre in a range of H-phosphonates can be assigned using a combination of chromatographic mobility,…”
Get full text

Exploration of conjugate addition routes to advanced tricyclic components of mangicol A by Pichlmair, Stefan, de Lera Ruiz, Manuel, Vilotijevic, Ivan, Paquette, Leo A.

“…Two synthetic approaches to the cytotoxic marine natural product known as mangicol A are described. The starting material common to both pathways is the…”
Get full text

Adenosine A2A Receptor as a Drug Discovery Target by de Lera Ruiz, Manuel, Lim, Yeon-Hee, Zheng, Junying

“…The adenosine A2A receptor is a G-protein-coupled receptor (GPCR) that has been extensively studied during the past few decades because it offers numerous…”
Get full text

Invention of MK-7845, a SARS-CoV‑2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic by Shurtleff, Valerie W., Layton, Mark E., Parish, Craig A., Perkins, James J., Schreier, John D., Wang, Yunyi, Adam, Gregory C., Alvarez, Nadine, Bahmanjah, Soheila, Bahnck-Teets, Carolyn M., Boyce, Christopher W., Burlein, Christine, Cabalu, Tamara D., Campbell, Brian T., Carroll, Steven S., Chang, Wonsuk, de Lera Ruiz, Manuel, Dolgov, Enriko, Fay, John F., Fox, Nicholas G., Goh, Shih Lin, Hartingh, Timothy J., Hurzy, Danielle M., Kelly, Michael J., Klein, Daniel J., Klingler, Franca-Maria, Krishnamurthy, Harini, Kudalkar, Shalley, Mayhood, Todd W., McKenna, Philip M., Murray, Edward M., Nahas, Debbie, Nawrat, Christopher C., Park, Steven, Qian, Dongming, Roecker, Anthony J., Sharma, Vijeta, Shipe, William D., Su, Jing, Taggart, Robert V., Truong, Quang, Wu, Yin, Zhou, Xiaoyan, Zhuang, Ningning, Perlin, David S., Olsen, David B., Howe, John A., McCauley, John A.

“…As SARS-CoV-2 continues to circulate, antiviral treatments are needed to complement vaccines. The virus’s main protease, 3CLPro, is an attractive drug target…”
Get full text

Adenosine A 2A Receptor as a Drug Discovery Target by de Lera Ruiz, Manuel, Lim, Yeon-Hee, Zheng, Junying

Get full text

Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity by de Lera Ruiz, Manuel, Zheng, Junying, Berlin, Michael Y., McCormick, Kevin D., Aslanian, Robert G., West, Robert, Hwa, Joyce, Lachowicz, Jean, van Heek, Margaret

“…A novel series of non-imidazole bicyclic and tricyclic histamine H3 receptor antagonists has been discovered. Compound 17 was identified as a centrally…”
Get full text

Evaluation of possible intramolecular [4+2] cycloaddition routes for assembling the central tetracyclic core of the potent marine antiinflammatory agent mangicol A by Pichlmair, Stefan, de Lera Ruiz, Manuel, Basu, Kallol, Paquette, Leo A.

“…A plan for enantioselective construction of the mangicol A framework by means of intramolecular Diels–Alder cycloaddition is outlined. First to be assembled is…”
Get full text

Cover Picture: Discovery of MK-8970: An Acetal Carbonate Prodrug of Raltegravir with Enhanced Colonic Absorption (ChemMedChem 2/2015) by Walji, Abbas M., Sanchez, Rosa I., Clas, Sophie-Dorothee, Nofsinger, Rebecca, de Lera Ruiz, Manuel, Li, Jing, Bennet, Amrithraj, John, Christopher, Bennett, David Jonathan, Sanders, John M., Di Marco, Christina N., Kim, Somang Hope, Balsells, Jaume, Ceglia, Scott S., Dang, Qun, Manser, Kimberly, Nissley, Becky, Wai, John S., Hafey, Michael, Wang, Junying, Chessen, Gene, Templeton, Allen, Higgins, John, Smith, Ronald, Wu, Yunhui, Grobler, Jay, Coleman, Paul J.

Get full text