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Your search keyword '"Abdellatif El Marrouni"' showing total 10 results
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10 results on '"Abdellatif El Marrouni"'

1. Total synthesis of putative 11-epi-lyngbouilloside aglycon

Author

Amandine Kolleth, Julian Gebauer, Abdellatif El Marrouni, Raphael Lebeuf, Celine Prevost, Eric Brohan, Stellios Arseniyadis, and Janine Cossy

Subjects
Total synthesis, RCM, Mukaiyama aldol, Lyngbouilloside, Lyngya bouillonii, Boeckman esterification, Chemistry, QD1-999
Abstract

We report here the total synthesis of 11-epi-lyngbouilloside aglycon. Our strategy features a Boeckman-type esterification followed by a RCM to form the 14-membered ring macrolactone and a late-stage side chain introduction via a Wittig olefination. Overall, the final product was obtained in 20 steps and 2% overall yield starting from commercially available 3-methyl-but-3-enol. Most importantly, the strategy employed is versatile enough to eventually allow us to complete the synthesis of the natural product and irrevocably confirm its structure.

Published
2016
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3. Potent targeted activator of cell kill molecules eliminate cells expressing HIV-1

Author

Carl J. Balibar, Daniel J. Klein, Beata Zamlynny, Tracy L. Diamond, Zhiyu Fang, Carol A. Cheney, Jan Kristoff, Meiqing Lu, Marina Bukhtiyarova, Yangsi Ou, Min Xu, Lei Ba, Steven S. Carroll, Abdellatif El Marrouni, John F. Fay, Ashley Forster, Shih Lin Goh, Meigang Gu, Daniel Krosky, Daniel I. S. Rosenbloom, Payal Sheth, Deping Wang, Guoxin Wu, Matthias Zebisch, Tian Zhao, Paul Zuck, Jay Grobler, Daria J. Hazuda, Bonnie J. Howell, and Antonella Converso

Subjects
General Medicine
Abstract

Antiretroviral therapy inhibits HIV-1 replication but is not curative due to establishment of a persistent reservoir after virus integration into the host genome. Reservoir reduction is therefore an important HIV-1 cure strategy. Some HIV-1 nonnucleoside reverse transcriptase inhibitors induce HIV-1 selective cytotoxicity in vitro but require concentrations far exceeding approved dosages. Focusing on this secondary activity, we found bifunctional compounds with HIV-1–infected cell kill potency at clinically achievable concentrations. These targeted activator of cell kill (TACK) molecules bind the reverse transcriptase–p66 domain of monomeric Gag-Pol and act as allosteric modulators to accelerate dimerization, resulting in HIV-1 + cell death through premature intracellular viral protease activation. TACK molecules retain potent antiviral activity and selectively eliminate infected CD4 + T cells isolated from people living with HIV-1, supporting an immune-independent clearance strategy.

Published
2023
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4. Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery

Author

W. Peter Wuelfing, Abdellatif El Marrouni, Maya P. Lipert, Pierre Daublain, Filippos Kesisoglou, Antonella Converso, and Allen C. Templeton

Subjects
Dose-Response Relationship, Drug, Pharmaceutical Preparations, Solubility, Chemistry, Pharmaceutical, Drug Discovery, Administration, Oral, Animals, Humans, Molecular Medicine, Oral Mucosal Absorption
Abstract

Small molecule developability challenges have been well documented over the last two decades. One of these critical developability parameters is aqueous solubility. In general, more soluble compounds have improved oral absorption. While enabling formulation technologies exist to improve bioperformance for low solubility compounds, these are often more complex, expensive, and challenging to scale up. Therefore, to avoid these development issues, medicinal chemists need tools to rapidly profile and improve the physicochemical properties of molecules during discovery. Dose number (Do) is a simple metric to predict whether a compound will be reasonably absorbed based on solubility at an expected clinical dose and represents a valuable parameter to the medicinal chemist defining a clinical candidate. The goal of this mini-Perspective is to present the background of the Do equation and how it can be effectively used to rapidly predict oral absorption potential for molecules in the discovery space.

Published
2022
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5. Activity of Tricyclic Pyrrolopyrimidine Gyrase B Inhibitor against Mycobacterium abscessus

Author

Abdeldjalil Madani, Dereje A. Negatu, Abdellatif El Marrouni, Randy R. Miller, Christopher Boyce, Nicholas Murgolo, Christopher J. Bungard, Matthew D. Zimmerman, Véronique Dartois, Martin Gengenbacher, David B. Olsen, and Thomas Dick

Subjects
Adenosine Triphosphatases, Pharmacology, Mycobacterium abscessus, Mycobacterium Infections, Nontuberculous, Nontuberculous Mycobacteria, Microbial Sensitivity Tests, Anti-Bacterial Agents, Mice, Pyrimidines, Infectious Diseases, DNA Gyrase, Animals, Pyrroles, Pharmacology (medical)
Abstract

Tricyclic pyrrolopyrimidines (TPPs) are a new class of antibacterials inhibiting the ATPase of DNA gyrase. TPP8, a representative of this class, is active against Mycobacterium abscessus in vitro. Spontaneous TPP8 resistance mutations mapped to the ATPase domain of M. abscessus DNA gyrase and the compound inhibited DNA supercoiling activity of recombinant M. abscessus enzyme. Further profiling of TPP8 in macrophage and mouse infection studies demonstrated proof-of-concept activity against M. abscessus ex vivo and in vivo.

Published
2022
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6. Current Status of Approaches to Eradicate <scp>HIV</scp> Infection

Author

Antonella Converso, Richard J. O. Barnard, David M. Tellers, Abdellatif El Marrouni, Scott E. Wolkenberg, and Tracy L. Diamond

Subjects
medicine.medical_specialty, Acquired immunodeficiency syndrome (AIDS), business.industry, Human immunodeficiency virus (HIV), Medicine, Current (fluid), business, Intensive care medicine, medicine.disease, medicine.disease_cause
Published
2021
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7. Synthesis of C6-Substituted Purine Nucleoside Analogues via Late-Stage Photoredox/Nickel Dual Catalytic Cross-Coupling

Author

Abdellatif El Marrouni, Alayna M. Johnson, James J. Perkins, and Valerie W Shurtleff

Subjects
chemistry.chemical_classification, Purine, Chemistry, Drug discovery, Organic Chemistry, Late stage, chemistry.chemical_element, Biochemistry, Combinatorial chemistry, Catalysis, Nickel, chemistry.chemical_compound, Drug Discovery, Nucleoside, Alkyl
Abstract

[Image: see text] Nucleoside analogues have been and continue to be extremely important compounds in drug discovery. Despite the significant effort dedicated to their synthesis, medicinal chemistry campaigns around these structures are often hampered by synthetic challenges. We describe a strategy for the functionalization of purine nucleosides via photoredox and nickel-catalyzed sp(2)–sp(3) cross-coupling. The conditions described herein allow for coupling of unprotected nucleosides with readily available alkyl bromides, providing opportunities for their application to parallel medicinal chemistry.

Published
2021

9. 2024 Medicinal Chemistry Reviews

Author

Thomas A. Baillie, Andrew G. Capacci, Nick A. Paras, Karin Worm, James L. Carr, Mia C. Callens, Ethan Chidlow, Tryfon Zarganes-Tzitzikas, Katherine S. England, Paul E. Brennan, Yonghong Song, Nicholas Wurtz, Kevin J. Filipski, Kentaro Futatsugi, Robert Dullea, Michelle R. Garnsey, Daniel J. Smaltz, Matthew M. Weiss, Jack A. Terrett, Huifen Chen, Marion Lanier, Samantha Evans, Gregory Williams, Joshua Wollam, Debra Brennan, Yufan Liang, Scott Mlynarski, Bing-Yan Zhu, David J. St. Jean, Trang Tieu, Angel Guzman-Perez, Alexander M. Taylor, Linjie Li, Chenxi Wang, Liuzhi Hu, Xiaowu Dong, Jinxin Che, Andrew S. Bell, James A. Brannigan, Kevin X. Rodriguez, Isaac D. Falk, Bradley T. Reid, Greta Klejborowska, Camilla Scarpellini, Caroline Lanthier, Koen Augustyns, Benjamin D. Sellers, Brian R. Hearn, Katerina Leftheris*, Jennifer X. Qiao, Abdellatif El Marrouni, Abbas Walji, Matthew A. Marx, Jill Hallin, James Christensen, Brad Fell, David W. Lin, Megan Armstrong, Jennifer Jiang, Juan del Pozo, Christiana N. Teijaro, Erika Araujo, Björn Bartels, Ian M. Be, Thomas A. Baillie, Andrew G. Capacci, Nick A. Paras, Karin Worm, James L. Carr, Mia C. Callens, Ethan Chidlow, Tryfon Zarganes-Tzitzikas, Katherine S. England, Paul E. Brennan, Yonghong Song, Nicholas Wurtz, Kevin J. Filipski, Kentaro Futatsugi, Robert Dullea, Michelle R. Garnsey, Daniel J. Smaltz, Matthew M. Weiss, Jack A. Terrett, Huifen Chen, Marion Lanier, Samantha Evans, Gregory Williams, Joshua Wollam, Debra Brennan, Yufan Liang, Scott Mlynarski, Bing-Yan Zhu, David J. St. Jean, Trang Tieu, Angel Guzman-Perez, Alexander M. Taylor, Linjie Li, Chenxi Wang, Liuzhi Hu, Xiaowu Dong, Jinxin Che, Andrew S. Bell, James A. Brannigan, Kevin X. Rodriguez, Isaac D. Falk, Bradley T. Reid, Greta Klejborowska, Camilla Scarpellini, Caroline Lanthier, Koen Augustyns, Benjamin D. Sellers, Brian R. Hearn, Katerina Leftheris*, Jennifer X. Qiao, Abdellatif El Marrouni, Abbas Walji, Matthew A. Marx, Jill Hallin, James Christensen, Brad Fell, David W. Lin, Megan Armstrong, Jennifer Jiang, Juan del Pozo, Christiana N. Teijaro, Erika Araujo, Björn Bartels, and Ian M. Be

10. ACS Medicinal Chemistry Reviews

Author

Joanne J. Bronson, Mark A. Murcko, Erin L. Cole, Lindsey R. Drake, Sanju Narayanan, Rajendra Uprety, Rangan Maitra, Scott Runyon, Wu Yang, James R. Corte, Joseph M. Luettgen, Zhi-Liang Wei, Danielle L. Aubele, Kelly A. Pike, Ramsay Beveridge, Patrick Cyr, Alex Skeldon, Li Wang, Jason D. Burch, Karin Worm, Jill Henault, Mark David Andrews, Marcel John de Groot, Kevin Neil Dack, Min Lu, Rachel L. Palte, Scott N. Mlynarski, Jason D. Shields, Oliver Schadt, Guangxiu Dai, Weiguo Xiang, Xin Han, Lijie Zhao, Shaomeng Wang, Thomas P. Stratton, Alexandre Mercier, Emma Abernathy, Jason Hudlicky, Lutete Peguy Khonde, Paul Jackson, Peter R. Hewitt, Oliver Barker, Matthew D. Helm, Xavier Jacq, Colin R. O'Dowd, Natalie Page, J. S. Shane Rountree, Timothy Harrison, Anmol Gulati, Xin Guo, Anton Delwig, Noriko Ishisoko, Robert A. Blake, Jose Raul Montero Bastidas, Abdellatif El Marrouni, Maria Irina Chiriac, Thomas Struble, Dipannita Kalyani, Jeffrey A. Dodge, Michael J. Chalmers, Howard Broughton, Alfonso Espada, Joshua A. Lees, Seungil Han, Gene M. Dubowchik, Robe, Joanne J. Bronson, Mark A. Murcko, Erin L. Cole, Lindsey R. Drake, Sanju Narayanan, Rajendra Uprety, Rangan Maitra, Scott Runyon, Wu Yang, James R. Corte, Joseph M. Luettgen, Zhi-Liang Wei, Danielle L. Aubele, Kelly A. Pike, Ramsay Beveridge, Patrick Cyr, Alex Skeldon, Li Wang, Jason D. Burch, Karin Worm, Jill Henault, Mark David Andrews, Marcel John de Groot, Kevin Neil Dack, Min Lu, Rachel L. Palte, Scott N. Mlynarski, Jason D. Shields, Oliver Schadt, Guangxiu Dai, Weiguo Xiang, Xin Han, Lijie Zhao, Shaomeng Wang, Thomas P. Stratton, Alexandre Mercier, Emma Abernathy, Jason Hudlicky, Lutete Peguy Khonde, Paul Jackson, Peter R. Hewitt, Oliver Barker, Matthew D. Helm, Xavier Jacq, Colin R. O'Dowd, Natalie Page, J. S. Shane Rountree, Timothy Harrison, Anmol Gulati, Xin Guo, Anton Delwig, Noriko Ishisoko, Robert A. Blake, Jose Raul Montero Bastidas, Abdellatif El Marrouni, Maria Irina Chiriac, Thomas Struble, Dipannita Kalyani, Jeffrey A. Dodge, Michael J. Chalmers, Howard Broughton, Alfonso Espada, Joshua A. Lees, Seungil Han, Gene M. Dubowchik, and Robe

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