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Miniaturized Modular Click Chemistry-enabled Rapid Discovery of Unique SARS-CoV-2 Mpro Inhibitors With Robust Potency and Drug-like Profile.
Yang M, Lee MK, Gao S, Song L, Jang HY, Jo I, Yang CC, Sylvester K, Ko C, Wang S, Ye B, Tang K, Li J, Gu M, Müller CE, Sträter N, Liu X, Kim M, Zhan P. Yang M, et al. Among authors: sylvester k. Adv Sci (Weinh). 2024 Nov;11(43):e2404884. doi: 10.1002/advs.202404884. Epub 2024 Sep 25. Adv Sci (Weinh). 2024. PMID: 39319611 Free PMC article.
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Gao S, Sylvester K, Song L, Claff T, Jing L, Woodson M, Weiße RH, Cheng Y, Schäkel L, Petry M, Gütschow M, Schiedel AC, Sträter N, Kang D, Xu S, Toth K, Tavis J, Tollefson AE, Müller CE, Liu X, Zhan P. Gao S, et al. Among authors: sylvester k. J Med Chem. 2022 Oct 13;65(19):13343-13364. doi: 10.1021/acs.jmedchem.2c01146. Epub 2022 Sep 15. J Med Chem. 2022. PMID: 36107752
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Gao S, Song L, Claff T, Woodson M, Sylvester K, Jing L, Weiße RH, Cheng Y, Sträter N, Schäkel L, Gütschow M, Ye B, Yang M, Zhang T, Kang D, Toth K, Tavis J, Tollefson AE, Müller CE, Zhan P, Liu X. Gao S, et al. Among authors: sylvester k. J Med Chem. 2022 Dec 22;65(24):16902-16917. doi: 10.1021/acs.jmedchem.2c01716. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475694
Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability.
Gao S, Song L, Sylvester K, Mercorelli B, Loregian A, Toth K, Weiße RH, Useini A, Sträter N, Yang M, Ye B, Tollefson AE, Müller CE, Liu X, Zhan P. Gao S, et al. Among authors: sylvester k. J Med Chem. 2023 Dec 14;66(23):16426-16440. doi: 10.1021/acs.jmedchem.3c01876. Epub 2023 Nov 22. J Med Chem. 2023. PMID: 37992202
Cathepsin-Targeting SARS-CoV-2 Inhibitors: Design, Synthesis, and Biological Activity.
Flury P, Breidenbach J, Krüger N, Voget R, Schäkel L, Si Y, Krasniqi V, Calistri S, Olfert M, Sylvester K, Rocha C, Ditzinger R, Rasch A, Pöhlmann S, Kronenberger T, Poso A, Rox K, Laufer SA, Müller CE, Gütschow M, Pillaiyar T. Flury P, et al. Among authors: sylvester k. ACS Pharmacol Transl Sci. 2024 Jan 19;7(2):493-514. doi: 10.1021/acsptsci.3c00313. eCollection 2024 Feb 9. ACS Pharmacol Transl Sci. 2024. PMID: 38357286
Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.
Pillaiyar T, Flury P, Krüger N, Su H, Schäkel L, Barbosa Da Silva E, Eppler O, Kronenberger T, Nie T, Luedtke S, Rocha C, Sylvester K, Petry MRI, McKerrow JH, Poso A, Pöhlmann S, Gütschow M, O'Donoghue AJ, Xu Y, Müller CE, Laufer SA. Pillaiyar T, et al. Among authors: sylvester k. J Med Chem. 2022 Jul 14;65(13):9376-9395. doi: 10.1021/acs.jmedchem.2c00636. Epub 2022 Jun 16. J Med Chem. 2022. PMID: 35709506
Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors.
Breidenbach J, Lemke C, Pillaiyar T, Schäkel L, Al Hamwi G, Diett M, Gedschold R, Geiger N, Lopez V, Mirza S, Namasivayam V, Schiedel AC, Sylvester K, Thimm D, Vielmuth C, Phuong Vu L, Zyulina M, Bodem J, Gütschow M, Müller CE. Breidenbach J, et al. Among authors: sylvester k. Angew Chem Int Ed Engl. 2021 Apr 26;60(18):10423-10429. doi: 10.1002/anie.202016961. Epub 2021 Mar 24. Angew Chem Int Ed Engl. 2021. PMID: 33655614 Free PMC article.
337 results