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75 Results       Page 1

 [1] 
American Chemical Society: Journal of Medicinal Chemistry
  original article Date Title Authors   All Authors
1 [GO] 2024―Jul―12 Amphiphilic Heparinoids as Potent Antiviral Agents against SARS-CoV-2 Mohit Chhabra, Chethan D. Shanthamurthy, Nanjudaswamy Vijendra Kumar, Sandhya Mardhekar, Sharath S. Vishweshwara, Norbert Wimmer, et al. (+13)
2 [GO] 2024―Jul―05 Fixing the Achilles Heel of Pfizer’s Paxlovid for COVID-19 Treatment Lennart Brewitz, Christopher J. Schofield
3 [GO] 2024―Jul―05 New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs Wenyi Zhang, Lecheng Xiao, Dianyang Li, Yuxuan Hu, Wenying Yu
4 [GO] 2024―Jul―02 Structure-Guided Design of Potent Coronavirus Inhibitors with a 2-Pyrrolidone Scaffold: Biochemical, Crystallographic, and Virological Studies Chamandi S. Dampalla, Yunjeong Kim, Alexandria Zabiegala, Dennis J. Howard, Harry Nhat Nguyen, Trent K. Madden, et al. (+7)
5 [GO] 2024―Jun―14 Correction to “Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead” N. G. R. Dayan Elshan, Karen C. Wolff, Laura Riva, Ashley K. Woods, Gennadii Grabovyi, Katy Wilson, et al. (+26)
6 [GO] 2024―Jun―12 Colloidal Aggregation Confounds Cell-Based Covid-19 Antiviral Screens Isabella S. Glenn, Lauren N. Hall, Mir M. Khalid, Melanie Ott, Brian K. Shoichet
7 [GO] 2024―May―30 Design, Synthesis, and Structure-Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors Arik J. Hone, Ulises Santiago, Peta J. Harvey, Bassel Tekarli, Joanna Gajewiak, David J. Craik, et al. (+2)
8 [GO] 2024―May―16 Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs Julian Breidenbach, Rabea Voget, Yaoyao Si, Alexandra Hingst, Tobias Claff, Katharina Sylvester, et al. (+8)
9 [GO] 2024―Apr―30 A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19 Charlotte M. N. Allerton, Joel T. Arcari, Lisa M. Aschenbrenner, Melissa Avery, Bruce M. Bechle, Mohammad Amin Behzadi, et al. (+41)
10 [GO] 2024―Apr―12 Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease Yugendar R. Alugubelli, Jing Xiao, Kaustav Khatua, Sathish Kumar, Long Sun, Yuying Ma, et al. (+9)
11 [GO] 2024―Apr―09 Discovery of 2-Amide-3-methylester Thiophenes that Target SARS-CoV-2 Mac1 and Repress Coronavirus Replication, Validating Mac1 as an Antiviral Target Sarah Wazir, Tomi A. O. Parviainen, Jessica J. Pfannenstiel, Men Thi Hoai Duong, Daniel Cluff, Sven T. Sowa, et al. (+6)
12 [GO] 2024―Feb―17 Invention of MK-7845, a SARS-CoV-2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic Valerie W. Shurtleff, Mark E. Layton, Craig A. Parish, James J. Perkins, John D. Schreier, Yunyi Wang, et al. (+42)
13 [GO] 2024―Feb―09 Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead N. G. R. Dayan Elshan, Karen C. Wolff, Laura Riva, Ashley K. Woods, Gennadii Grabovyi, Katy Wilson, et al. (+25)
14 [GO] 2023―Nov―22 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 Shenghua Gao, Letian Song, Katharina Sylvester, Beatrice Mercorelli, Arianna Loregian, Karoly Toth, et al. (+9)
15 [GO] 2023―Oct―30 Mapping the Lipid Signatures in COVID-19 Infection: Diagnostic and Therapeutic Solutions Aishi Dasgupta, Shon Gangai, Rishikesh Narayan, Shobhna Kapoor
16 [GO] 2023―Oct―26 Clinical Translation of Aptamers for COVID-19 Yang Zhang, Yongen Li
17 [GO] 2023―Sep―27 Structure-Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties Kohei Tsuji, Takahiro Ishii, Takuya Kobayakawa, Nobuyo Higashi-Kuwata, Kouki Shinohara, Chika Azuma, et al. (+7)
18 [GO] 2023―Aug―19 Discovery of GS-5245 (Obeldesivir), an Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys Richard L. Mackman, Rao V. Kalla, Darius Babusis, Jared Pitts, Kimberly T. Barrett, Kwon Chun, et al. (+28)
19 [GO] 2023―Aug―18 Discovery and Mechanism Study of SARS-CoV-2 3C-like Protease Inhibitors with a New Reactive Group Pengxuan Ren, Hui Li, Tianqing Nie, Xiaoqin Jian, Changyue Yu, Jian Li, et al. (+10)
20 [GO] 2023―Aug―18 Alkyne as a Latent Warhead to Covalently Target SARS-CoV-2 Main Protease Chau Ngo, William Fried, Saba Aliyari, Joshua Feng, Chao Qin, Shilei Zhang, et al. (+6)
21 [GO] 2023―Aug―10 A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease Zhi Zachary Geng, Sandeep Atla, Namir Shaabani, Veerabhadra Vulupala, Kai S. Yang, Yugendar R. Alugubelli, et al. (+12)
22 [GO] 2023―Jul―20 C-2 Thiophenyl Tryptophan Trimers Inhibit Cellular Entry of SARS-CoV-2 through Interaction with the Viral Spike (S) Protein Marta Gargantilla, Clara Francés, Anmol Adhav, Alicia Forcada-Nadal, Belén Martínez-Gualda, Olaia Martí-Marí, et al. (+16)
23 [GO] 2023―Jun―09 Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase Isha Singh, Fengling Li, Elissa A. Fink, Irene Chau, Alice Li, Annía Rodriguez-Hernández, et al. (+17)
24 [GO] 2023―Apr―11 1-O-Octadecyl-2-O-benzyl-sn-glyceryl-3-phospho-GS-441524 (V2043). Evaluation of Oral V2043 in a Mouse Model of SARS-CoV-2 Infection and Synthesis and Antiviral Evaluation of Additional Phospholipid Esters with Enhanced Anti-SARS-CoV-2 Activity Aaron F. Carlin, James R. Beadle, Alex E. Clark, Kendra L. Gully, Fernando R. Moreira, Ralph S. Baric, et al. (+13)
25 [GO] 2023―Feb―09 Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine Lennart Brewitz, Leo Dumjahn, Yilin Zhao, C. David Owen, Stephen M. Laidlaw, Tika R. Malla, et al. (+10)
26 [GO] 2023―Jan―10 Self-Adjuvanting Protein Vaccine Conjugated with a Novel Synthetic TLR4 Agonist on Virus-Like Liposome Induces Potent Immunity against SARS-CoV-2 Dong Ding, Yu Wen, Chun-Miao Liao, Xu-Guang Yin, Ru-Yan Zhang, Jian Wang, et al. (+7)
27 [GO] 2022―Dec―12 Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2 Wenying Yu, Yucheng Zhao, Hui Ye, Nanping Wu, Yixian Liao, Nannan Chen, et al. (+6)
28 [GO] 2022―Dec―07 Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors Shenghua Gao, Letian Song, Tobias Claff, Molly Woodson, Katharina Sylvester, Lanlan Jing, et al. (+15)
29 [GO] 2022―Nov―10 Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen Jiao Li, Fumei Zhong, Mingwei Li, Yaqian Liu, Lei Wang, Mingqing Liu, et al. (+8)
30 [GO] 2022―Oct―14 Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease Yuya Hirose, Naoya Shindo, Makiko Mori, Satsuki Onitsuka, Hikaru Isogai, Rui Hamada, et al. (+15)
31 [GO] 2022―Sep―30 Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease Mark S. Cooper, Linlin Zhang, Mohamed Ibrahim, Kaixuan Zhang, Xinyuanyuan Sun, Judith Röske, et al. (+12)
32 [GO] 2022―Sep―28 Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure-Activity Relationship Insights and Evolution Perspectives Gabriele La Monica, Alessia Bono, Antonino Lauria, Annamaria Martorana
33 [GO] 2022―Sep―15 Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity Shenghua Gao, Katharina Sylvester, Letian Song, Tobias Claff, Lanlan Jing, Molly Woodson, et al. (+15)
34 [GO] 2022―Jun―22 Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir Kai S. Yang, Sunshine Z. Leeuwon, Shiqing Xu, Wenshe Ray Liu
35 [GO] 2022―Jun―16 Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination Thanigaimalai Pillaiyar, Philipp Flury, Nadine Krüger, Haixia Su, Laura Schäkel, Elany Barbosa Da Silva, et al. (+15)
36 [GO] 2022―May―31 Structure-Guided Design of Potent Spirocyclic Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3C-like Protease Chamandi S. Dampalla, Athri D. Rathnayake, Anushka C. Galasiti Kankanamalage, Yunjeong Kim, Krishani Dinali Perera, Harry Nhat Nguyen, et al. (+10)
37 [GO] 2022―May―27 Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease Haozhou Tan, Yanmei Hu, Prakash Jadhav, Bin Tan, Jun Wang
38 [GO] 2022―May―12 Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine Tika R. Malla, Lennart Brewitz, Dorian-Gabriel Muntean, Hiba Aslam, C. David Owen, Eidarus Salah, et al. (+6)
39 [GO] 2022―May―04 S-217622, a 3CL Protease Inhibitor and Clinical Candidate for SARS-CoV-2 Joel D. A. Tyndall
40 [GO] 2022―Apr―19 Potent Inhibition of SARS-CoV-2 nsp14 N7-Methyltransferase by Sulfonamide-Based Bisubstrate Analogues Rostom Ahmed-Belkacem, Marcel Hausdorff, Adrien Delpal, Priscila Sutto-Ortiz, Agathe M. G. Colmant, Franck Touret, et al. (+7)
41 [GO] 2022―Mar―30 Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19 Yuto Unoh, Shota Uehara, Kenji Nakahara, Haruaki Nobori, Yukiko Yamatsu, Shiho Yamamoto, et al. (+19)
42 [GO] 2022―Feb―09 Advances Toward COVID-19 Therapies Special Issue Nouri Neamati
43 [GO] 2022―Feb―02 MPLA-Adjuvanted Liposomes Encapsulating S-Trimer or RBD or S1, but Not S-ECD, Elicit Robust Neutralization Against SARS-CoV-2 and Variants of Concern Jian Wang, Xu-Guang Yin, Yu Wen, Jie Lu, Ru-Yan Zhang, Shi-Hao Zhou, et al. (+3)
44 [GO] 2022―Jan―24 Self-Adjuvanting Lipoprotein Conjugate αGalCer-RBD Induces Potent Immunity against SARS-CoV-2 and its Variants of Concern Jian Wang, Yu Wen, Shi-Hao Zhou, Hai-Wei Zhang, Xiao-Qian Peng, Ru-Yan Zhang, et al. (+5)
45 [GO] 2022―Jan―04 Design and Evaluation of a Novel Peptide-Drug Conjugate Covalently Targeting SARS-CoV-2 Papain-like Protease Na Liu, Yichi Zhang, Yingshou Lei, Rui Wang, Meimiao Zhan, Jianbo Liu, et al. (+5)
46 [GO] 2021―Dec―05 Structure-Guided Design of Potent Inhibitors of SARS-CoV-2 3CL Protease: Structural, Biochemical, and Cell-Based Studies Chamandi S. Dampalla, Athri D. Rathnayake, Krishani Dinali Perera, Abdul-Rahman M. Jesri, Harry Nhat Nguyen, Matthew J. Miller, et al. (+9)
47 [GO] 2021―Nov―24 Stapled Peptides Targeting SARS-CoV-2 Spike Protein HR1 Inhibit the Fusion of Virus to Its Cell Receptor Mengjun Zheng, Wei Cong, Haoran Peng, Jie Qing, Huaxing Shen, Yaxin Tang, et al. (+6)
48 [GO] 2021―Nov―23 Colloidal Aggregators in Biochemical SARS-CoV-2 Repurposing Screens Henry R. O’Donnell, Tia A. Tummino, Conner Bardine, Charles S. Craik, Brian K. Shoichet
49 [GO] 2021―Nov―20 Perspectives on SARS-CoV-2 Main Protease Inhibitors Kaifu Gao, Rui Wang, Jiahui Chen, Jetze J. Tepe, Faqing Huang, Guo-Wei Wei
50 [GO] 2021―Oct―27 Structural, Electronic, and Electrostatic Determinants for Inhibitor Binding to Subsites S1 and S2 in SARS-CoV-2 Main Protease Daniel W. Kneller, Hui Li, Stephanie Galanie, Gwyndalyn Phillips, Audrey Labbé, Kevin L. Weiss, et al. (+11)
51 [GO] 2021―Oct―21 Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity Zhengnan Shen, Kiira Ratia, Laura Cooper, Deyu Kong, Hyun Lee, Youngjin Kwon, et al. (+7)
52 [GO] 2021―Oct―09 Computational Design of Potent D-Peptide Inhibitors of SARS-CoV-2 Pedro A. Valiente, Han Wen, Satra Nim, JinAh Lee, Hyeon Ju Kim, Jinhee Kim, et al. (+6)
53 [GO] 2021―Sep―27 Discovery and Mechanism of SARS-CoV-2 Main Protease Inhibitors Sarah Huff, Indrasena Reddy Kummetha, Shashi Kant Tiwari, Matthew B. Huante, Alex E. Clark, Shaobo Wang, et al. (+5)
54 [GO] 2021―Sep―17 Synthetic Neutralizing Peptides Inhibit the Host Cell Binding of Spike Protein and Block Infection of SARS-CoV-2 Tao Wang, Xiaocui Fang, Tao Wen, Jian Liu, Zhaoyi Zhai, Zhiyou Wang, et al. (+4)
55 [GO] 2021―Sep―16 Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies Arun K. Ghosh, Jakka Raghavaiah, Dana Shahabi, Monika Yadav, Brandon J. Anson, Emma K. Lendy, et al. (+4)
56 [GO] 2021―Aug―04 Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CLpro) Sang Hoon Han, Christopher M. Goins, Tarun Arya, Woo-Jin Shin, Joshua Maw, Alice Hooper, et al. (+13)
57 [GO] 2021―Jul―30 Synthetic Peptides That Antagonize the Angiotensin-Converting Enzyme-2 (ACE-2) Interaction with SARS-CoV-2 Receptor Binding Spike Protein Afsaneh Sadremomtaz, Zayana M. Al-Dahmani, Angel J. Ruiz-Moreno, Alessandra Monti, Chao Wang, Taha Azad, et al. (+9)
58 [GO] 2021―Jul―19 Potent Neutralizing Antibodies Elicited by RBD-Fc-Based COVID-19 Vaccine Candidate Adjuvanted by the Th2-Skewing iNKT Cell Agonist Xi-Feng Wang, Meng-Jia Zhang, Na He, Ya-Cong Wang, Cheng Yan, Xiang-Zhao Chen, et al. (+4)
59 [GO] 2021―Jul―09 Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability Bing Bai, Alexandr Belovodskiy, Mostofa Hena, Appan Srinivas Kandadai, Michael A. Joyce, Holly A. Saffran, et al. (+20)
60 [GO] 2021―Jul―02 Structure-Guided Design of Conformationally Constrained Cyclohexane Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3CL Protease Chamandi S. Dampalla, Yunjeong Kim, Naemi Bickmeier, Athri D. Rathnayake, Harry Nhat Nguyen, Jian Zheng, et al. (+7)
61 [GO] 2021―Apr―23 Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors Naoya Kitamura, Michael Dominic Sacco, Chunlong Ma, Yanmei Hu, Julia Alma Townsend, Xiangzhi Meng, et al. (+11)
62 [GO] 2021―Apr―22 Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease Annelies Stevaert, Besir Krasniqi, Benjamin Van Loy, Tien Nguyen, Joice Thomas, Julie Vandeput, et al. (+6)
63 [GO] 2021―Apr―19 Design, Synthesis, and Biological Evaluation of Peptidomimetic Aldehydes as Broad-Spectrum Inhibitors against Enterovirus and SARS-CoV-2 Wenhao Dai, Dirk Jochmans, Hang Xie, Hang Yang, Jian Li, Haixia Su, et al. (+12)
64 [GO] 2021―Apr―15 Insights into SARS-CoV-2’s Mutations for Evading Human Antibodies: Sacrifice and Survival Binquan Luan, Tien Huynh
65 [GO] 2021―Mar―23 Direct Observation of Protonation State Modulation in SARS-CoV-2 Main Protease upon Inhibitor Binding with Neutron Crystallography Daniel W. Kneller, Gwyndalyn Phillips, Kevin L. Weiss, Qiu Zhang, Leighton Coates, Andrey Kovalevsky
66 [GO] 2021―Feb―03 Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models Yingjun Li, Liu Cao, Ge Li, Feng Cong, Yunfeng Li, Jing Sun, et al. (+10)
67 [GO] 2020―Dec―02 Advances toward COVID-19 Therapies Special Issue Call for Papers Hong Liu, Nouri Neamati, Nicholas Meanwell, Wendy Young, Gunda I. Georg, Shaomeng Wang
68 [GO] 2020―Nov―13 Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities Rolando Cannalire, Carmen Cerchia, Andrea R. Beccari, Francesco Saverio Di Leva, Vincenzo Summa
69 [GO] 2020―Oct―15 Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19 Robert L. Hoffman, Robert S. Kania, Mary A. Brothers, Jay F. Davies, Rose A. Ferre, Ketan S. Gajiwala, et al. (+18)
70 [GO] 2020―Aug―26 Chinese therapeutic strategy for fighting COVID-19 and potential small-molecule inhibitors against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) Namrta Choudhry, Xin Zhao, Dan Xu, Mark Zanin, Weisan Chen, Zi-Feng Yang, Jianxin Chen
71 [GO] 2020―Jul―21 Lung protection by cathepsin C inhibition: a new hope for COVID-19 and ARDS? Brice Korkmaz, Adam Lesner, sylvain marchand-adam, Celia Moss, Dieter Erich Jenne
72 [GO] 2020―Jun―15 Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities Siyu Xiu, alexej dick, Han Ju, Sako Mirzaie, Fatemeh Abdi, Simon Cocklin, et al. (+2)
73 [GO] 2020―Jun―08 COVID-19: Drug targets and potential treatments Carmen Gil, Tiziana Ginex, Ines Maestro, Vanesa Nozal, Lucia Barrado-Gil, Miguel A. Cuesta-Geijo, et al. (+5)
74 [GO] 2020―Feb―27 Structure-based stabilization of non-native protein-protein interactions of coronavirus nucleocapsid proteins in antiviral drug design Shan-Meng Lin, Shih-Chao Lin, Jia-Ning Hsu, Chung-ke Chang, Ching-Ming Chien, Yong-Sheng Wang, et al. (+4)
75 [GO] 2020―Feb―11 Alpha-ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication Structure-based design, synthesis, and activity assessment Linlin Zhang, Daizong Lin, Yuri Kusov, Yong Nian, Qingjun Ma, Jiang Wang, et al. (+8)
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75 Results       Page 1


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