Diphenyl[(S)-pyrrolidin-3-yl]acetonitrile - PMC

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Select item 64993891.

Probing Structural Requirements for Human Topoisomerase I Inhibition by a Novel N1-Biphenyl Fluoroquinolone

Justine L. Delgado, Sarah R.C. Lentz, Chaitanya A. Kulkarni, Pratik R. Chheda, Hailey A. Held, Hiroshi Hiasa, Robert J. Kerns

Eur J Med Chem. Author manuscript; available in PMC 2020 Jun 15.

Published in final edited form as: Eur J Med Chem. 2019 Jun 15; 172: 109–130. Published online 2019 Mar 20. doi: 10.1016/j.ejmech.2019.03.040

PMCID:: PMC6499389

Abstract Article PDF–1.6M

Select item 73319402.

Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase

Arturo L. Aguirre, Pratik R. Chheda, Sarah R.C. Lentz, Hailey A. Held, Natalie P. Groves, Hiroshi Hiasa, Robert J. Kerns

Bioorg Med Chem. Author manuscript; available in PMC 2021 May 15.

Published in final edited form as: Bioorg Med Chem. 2020 May 15; 28(10): 115439. Published online 2020 Mar 13. doi: 10.1016/j.bmc.2020.115439

PMCID:: PMC7331940

Abstract Article PDF–2.4M

Select item 41405963.

Identification of Neuropeptide S Antagonists: Structure–Activity Relationship Studies, X-ray Crystallography, and in Vivo Evaluation

Carla Hassler, Yanan Zhang, Brian Gilmour, Tyler Graf, Timothy Fennell, Rodney Snyder, Jeffrey R. Deschamps, Rainer K. Reinscheid, Celia Garau, Scott P. Runyon

ACS Chem Neurosci. 2014 Aug 20; 5(8): 731–744. Published online 2014 Jun 25. doi: 10.1021/cn500113c

PMCID:: PMC4140596

Abstract Article PDF–1.1M

Select item 110918284.

Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D₃ (D₃R) and μ-Opioid (MOR) Receptors Ligands as Potentially Safer Analgesics

Alessandro Bonifazi, Elizabeth Saab, Julie Sanchez, Antonina L. Nazarova, Saheem A. Zaidi, Khorshada Jahan, Vsevolod Katritch, Meritxell Canals, J. Robert Lane, Amy Hauck Newman

J Med Chem. Author manuscript; available in PMC 2024 May 14.

Published in final edited form as: J Med Chem. 2023 Aug 10; 66(15): 10304–10341. Published online 2023 Jul 19. doi: 10.1021/acs.jmedchem.3c00417

PMCID:: PMC11091828

Abstract Article PDF–4.5M

Select item 74584275.

Sustainable Synthesis of a Potent and Selective 5-HT₇ Receptor Antagonist Using a Mechanochemical Approach

Vittorio Canale, Valeria Frisi, Xavier Bantreil, Frédéric Lamaty, Paweł Zajdel

J Org Chem. 2020 Aug 21; 85(16): 10958–10965. Published online 2020 Jul 24. doi: 10.1021/acs.joc.0c01044

PMCID:: PMC7458427

Abstract Article PDF–1.5M

Select item 88777246.

Synthesis of Guaianolide Analogs with a Tunable α-Methylene-γ-Lactam Electrophile and Correlating Bioactivity with Thiol Reactivity

Paul A. Jackson, Henry A. M. Schares, Katherine F. M. Jones, John C. Widen, Daniel P. Dempe, Francois Grillet, Matthew E. Cuellar, Michael A. Walters, Daniel A. Harki, Kay M. Brummond

J Med Chem. Author manuscript; available in PMC 2022 Feb 25.

Published in final edited form as: J Med Chem. 2020 Dec 10; 63(23): 14951–14978. Published online 2020 Nov 17. doi: 10.1021/acs.jmedchem.0c01464

PMCID:: PMC8877724

Abstract Article PDF–1.6M

Select item 69803557.

Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase

Logan D. Andrews, Timothy R. Kane, Paola Dozzo, Cat M. Haglund, Darin J. Hilderbrandt, Martin S. Linsell, Timothy Machajewski, Glen McEnroe, Alisa W. Serio, Kenneth B. Wlasichuk, David B. Neau, Svetlana Pakhomova, Grover L. Waldrop, Marc Sharp, Joe Pogliano, Ryan T. Cirz, Frederick Cohen

J Med Chem. Author manuscript; available in PMC 2020 Jan 24.

Published in final edited form as: J Med Chem. 2019 Aug 22; 62(16): 7489–7505. Published online 2019 Aug 9. doi: 10.1021/acs.jmedchem.9b00625

PMCID:: PMC6980355

Abstract Article PDF–1.5M

Select item 73839318.

Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes

Andrew S. Bell, Zhiyong Yu, Jennie A. Hutton, Megan H. Wright, James A. Brannigan, Daniel Paape, Shirley M. Roberts, Charlotte L. Sutherell, Markus Ritzefeld, Anthony J. Wilkinson, Deborah F. Smith, Robin J. Leatherbarrow, Edward W. Tate

J Med Chem. 2020 Jul 23; 63(14): 7740–7765. Published online 2020 Jun 24. doi: 10.1021/acs.jmedchem.0c00570

PMCID:: PMC7383931

Abstract Article PDF–3.9M

Select item 112474999.

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy

Godwin Akpeko Dziwornu, Donald Seanego, Stephen Fienberg, Monica Clements, Jasmin Ferreira, Venkata S. Sypu, Sauvik Samanta, Ashlyn D. Bhana, Constance M. Korkor, Larnelle F. Garnie, Nicole Teixeira, Kathryn J. Wicht, Dale Taylor, Ronald Olckers, Mathew Njoroge, Liezl Gibhard, Nicolaas Salomane, Sergio Wittlin, Rohit Mahato, Arnish Chakraborty, Nicole Sevilleno, Rachael Coyle, Marcus C. S. Lee, Luiz C. Godoy, Charisse Flerida Pasaje, Jacquin C. Niles, Janette Reader, Mariette van der Watt, Lyn-Marié Birkholtz, Judith M. Bolscher, Marloes H. C. de Bruijni, Lauren B. Coulson, Gregory S. Basarab, Sandeep R. Ghorpade, Kelly Chibale

J Med Chem. 2024 Jul 11; 67(13): 11401–11420. Published online 2024 Jun 25. doi: 10.1021/acs.jmedchem.4c01154

PMCID:: PMC11247499

Abstract Article PDF–4.4M

Select item 476643910.

Discovery of novel PDE9 inhibitors capable of inhibiting Aβ aggregation as potential candidates for the treatment of Alzheimer’s disease

Tao Su, Tianhua Zhang, Shishun Xie, Jun Yan, Yinuo Wu, Xingshu Li, Ling Huang, Hai-Bin Luo

Sci Rep. 2016; 6: 21826. Published online 2016 Feb 25. doi: 10.1038/srep21826

PMCID:: PMC4766439

Abstract Article PDF–2.9M

Select item 888140111.

Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y₁₄R Antagonist

Zhiwei Wen, Veronica Salmaso, Young-Hwan Jung, Ngan B. Phung, Varun Gopinatth, Qasim Shah, Alexandra T. Patterson, John C. R. Randle, Zhoumou Chen, Daniela Salvemini, David I. Lieberman, Gregory S. Whitehead, Tadeusz P. Karcz, Donald N. Cook, Kenneth A. Jacobson

J Med Chem. Author manuscript; available in PMC 2023 Feb 24.

Published in final edited form as: J Med Chem. 2022 Feb 24; 65(4): 3434–3459. Published online 2022 Feb 3. doi: 10.1021/acs.jmedchem.1c01964

PMCID:: PMC8881401

Abstract Article PDF–2.8M

Select item 638535812.

Discovery of ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureidyl derivatives as selective non-steroidal agonists of the G-protein coupled bile acid receptor-1

Francesco Saverio Di Leva, Carmen Festa, Adriana Carino, Simona De Marino, Silvia Marchianò, Daniele Di Marino, Claudia Finamore, Maria Chiara Monti, Angela Zampella, Stefano Fiorucci, Vittorio Limongelli

Sci Rep. 2019; 9: 2504. Published online 2019 Feb 21. doi: 10.1038/s41598-019-38840-z

PMCID:: PMC6385358

Abstract Article PDF–1.3M

Select item 1098299913.

Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs

Rishi R. Shah, Elena De Vita, Preethi S. Sathyamurthi, Daniel Conole, Xinyue Zhang, Elliot Fellows, Eleanor R. Dickinson, Carlos M. Fleites, Markus A. Queisser, John D. Harling, Edward W. Tate

J Med Chem. 2024 Mar 28; 67(6): 4641–4654. Published online 2024 Mar 13. doi: 10.1021/acs.jmedchem.3c02123