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Items: 1 to 20 of 236

1.
Discovery of Novel Inhibitors of Uridine Diphosphate-N-Acetylenolpyruvylglucosamine Reductase (MurB) from Pseudomonas aeruginosa, an Opportunistic Infectious Agent Causing Death in Cystic Fibrosis Patients
Marta Acebrón-García-de-Eulate, Joan Mayol-Llinàs, Matthew T. O. Holland, So Yeon Kim, Karen P. Brown, Chiara Marchetti, Jeannine Hess, Ornella Di Pietro, Vitor Mendes, Chris Abell, R. Andres Floto, Anthony G. Coyne, Tom L. Blundell
J Med Chem. Author manuscript; available in PMC 2023 Jul 25.
Published in final edited form as: J Med Chem. 2022 Feb 10; 65(3): 2149–2173. Published online 2022 Jan 26. doi: 10.1021/acs.jmedchem.1c01684
PMCID:
PMC7614804
AbstractArticlePDF–2.6M
2.
Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth
Peter C. Ray, Margaret Huggett, Penelope A. Turner, Malcolm Taylor, Laura A. T. Cleghorn, Julie Early, Anuradha Kumar, Shilah A. Bonnett, Lindsay Flint, Douglas Joerss, James Johnson, Aaron Korkegian, Steven Mullen, Abraham L. Moure, Susan H. Davis, Dinakaran Murugesan, Michael Mathieson, Nicola Caldwell, Curtis A. Engelhart, Dirk Schnappinger, Ola Epemolu, Fabio Zuccotto, Jennifer Riley, Paul Scullion, Laste Stojanovski, Lisa Massoudi, Gregory T. Robertson, Anne J. Lenaerts, Gail Freiberg, Dale J. Kempf, Thierry Masquelin, Philip A. Hipskind, Joshua Odingo, Kevin D. Read, Simon R. Green, Paul G. Wyatt, Tanya Parish
ACS Omega. 2021 Jan 26; 6(3): 2284–2311. Published online 2021 Jan 13. doi: 10.1021/acsomega.0c05589
PMCID:
PMC7841955
AbstractArticlePDF–1.9M
3.
Discovery of trisubstituted pyrazolines as a novel scaffold for the development of selective phosphodiesterase 5 inhibitors
Mohammad Abdel-Halim, Heather Tinsley, Adam B. Keeton, Mohammed Weam, Noha H. Atta, Mennatallah A. Hammam, Amr Hefnawy, Rolf W. Hartmann, Matthias Engel, Gary A. Piazza, Ashraf H. Abadi
Bioorg Chem. Author manuscript; available in PMC 2021 Nov 1.
Published in final edited form as: Bioorg Chem. 2020 Nov; 104: 104322. Published online 2020 Sep 28. doi: 10.1016/j.bioorg.2020.104322
PMCID:
PMC7686114
AbstractArticlePDF–1.0M
4.
Synthesis of Anti-Inflammatory Spirostene-Pyrazole Conjugates by a Consecutive Multicomponent Reaction of Diosgenin with Oxalyl Chloride, Arylalkynes and Hydrazines or Hydrazones
Maksim E. Mironov, Sergey A. Borisov, Tatyana V. Rybalova, Dmitry S. Baev, Tatyana G. Tolstikova, Elvira E. Shults
Molecules. 2022 Jan; 27(1): 162. Published online 2021 Dec 28. doi: 10.3390/molecules27010162
PMCID:
PMC8746855
AbstractArticlePDF–5.4M
5.
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties
Ganesha Rai, Daniel J. Urban, Bryan T. Mott, Xin Hu, Shyh-Ming Yang, Gloria A. Benavides, Michelle S. Johnson, Giuseppe L. Squadrito, Kyle R. Brimacombe, Tobie D. Lee, Dorian M. Cheff, Hu Zhu, Mark J. Henderson, Katherine Pohida, Gary A. Sulikowski, David M. Dranow, Md Kabir, Pranav Shah, Elias Padilha, Dingyin Tao, Yuhong Fang, Plamen P. Christov, Kwangho Kim, Somnath Jana, Pavan Muttil, Tamara Anderson, Nitesh K. Kunda, Helen J. Hathaway, Donna F. Kusewitt, Nobu Oshima, Murali Cherukuri, Douglas R. Davies, Jeffrey P. Norenberg, Larry A. Sklar, William J. Moore, Chi V. Dang, Gordon M. Stott, Leonard Neckers, Andrew J. Flint, Victor M. Darley-Usmar, Anton Simeonov, Alex G. Waterson, Ajit Jadhav, Matthew D. Hall, David J. Maloney
J Med Chem. Author manuscript; available in PMC 2021 Jan 25.
Published in final edited form as: J Med Chem. 2020 Oct 8; 63(19): 10984–11011. Published online 2020 Sep 27. doi: 10.1021/acs.jmedchem.0c00916
PMCID:
PMC7830743
AbstractArticlePDF–2.4M
6.
Access and Modulation of Substituted Pyrrolo[3,4-c]pyrazole-4,6-(2H,5H)-diones
Abdelaziz Ejjoummany, Jonathan Elie, Ahmed El Hakmaoui, Mohamed Akssira, Sylvain Routier, Frédéric Buron
Molecules. 2023 Aug; 28(15): 5811. Published online 2023 Aug 1. doi: 10.3390/molecules28155811
PMCID:
PMC10421423
AbstractArticlePDF–4.9M
7.
Discovery of 4,5-Dihydro-1H-thieno[2′,3′:2,3]thiepino [4,5-c]pyrazole-3-carboxamide Derivatives as the Potential Epidermal Growth Factor Receptors for Tyrosine Kinase Inhibitors
Jia Ke, Qi Lu, Xin Wang, Rui Sun, Zhe Jin, Xiaoyi Zhan, Jianshu Hu, David Chi-cheong Wan, Chun Hu
Molecules. 2018 Aug; 23(8): 1980. Published online 2018 Aug 8. doi: 10.3390/molecules23081980
PMCID:
PMC6222878
AbstractArticlePDF–1.4M
8.
Synthesis and Characterization of Some New Bis-Pyrazolyl-Thiazoles Incorporating the Thiophene Moiety as Potent Anti-Tumor Agents
Sobhi M. Gomha, Mastoura M. Edrees, Farag M. A. Altalbawy
Int J Mol Sci. 2016 Sep; 17(9): 1499. Published online 2016 Sep 7. doi: 10.3390/ijms17091499
PMCID:
PMC5037776
AbstractArticlePDF–864K
9.
Design and Synthesis of Novel Antimicrobial Acyclic and Heterocyclic Dyes and Their Precursors for Dyeing and/or Textile Finishing Based on 2-N-Acylamino-4,5,6,7-tetrahydro-benzo[b]thiophene Systems
Hoda Zaki Shams, Rafat Milad Mohareb, Maher Helmy Helal, Amira El-Sayed Mahmoud
Molecules. 2011 Aug; 16(8): 6271–6305. Published online 2011 Jul 26. doi: 10.3390/molecules16086271
PMCID:
PMC6264743
AbstractArticlePDF–587K
10.
Synthesis of New Azetidine and Oxetane Amino Acid Derivatives through Aza-Michael Addition of NH-Heterocycles with Methyl 2-(Azetidin- or Oxetan-3-Ylidene)Acetates
Emilis Gudelis, Sonata Krikštolaitytė, Monika Stančiauskaitė, Urtė Šachlevičiūtė, Aurimas Bieliauskas, Vaida Milišiūnaitė, Rokas Jankauskas, Neringa Kleizienė, Frank A. Sløk, Algirdas Šačkus
Molecules. 2023 Feb; 28(3): 1091. Published online 2023 Jan 21. doi: 10.3390/molecules28031091
PMCID:
PMC9921373
AbstractArticlePDF–1.7M
11.
Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives
Diana Becerra, Rodrigo Abonia, Juan-Carlos Castillo
Molecules. 2022 Aug; 27(15): 4723. Published online 2022 Jul 23. doi: 10.3390/molecules27154723
PMCID:
PMC9331265
AbstractArticlePDF–26M
12.
Design, Synthesis, Biological Evaluation and In Silico Studies of Pyrazole-Based NH2-Acyl Oseltamivir Analogues as Potent Neuraminidase Inhibitors
Jiqing Ye, Lin Lin, Jinyi Xu, Paul Kay-sheung Chan, Xiao Yang, Cong Ma
Pharmaceuticals (Basel) 2021 Apr; 14(4): 371. Published online 2021 Apr 16. doi: 10.3390/ph14040371
PMCID:
PMC8073777
AbstractArticlePDF–8.6M
13.
Synthesis and Characterization of Novel Methyl (3)5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates
Gita Matulevičiūtė, Eglė Arbačiauskienė, Neringa Kleizienė, Vilija Kederienė, Greta Ragaitė, Miglė Dagilienė, Aurimas Bieliauskas, Vaida Milišiūnaitė, Frank A. Sløk, Algirdas Šačkus
Molecules. 2021 Jul; 26(13): 3808. Published online 2021 Jun 22. doi: 10.3390/molecules26133808
PMCID:
PMC8270337
AbstractArticlePDF–15M
14.
Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities
Mohamed Ramadan, Ashraf A. Aly, Lamiaa E. Abd El-Haleem, Mohammed B. Alshammari, Stefan Bräse
Molecules. 2021 Aug; 26(16): 4995. Published online 2021 Aug 18. doi: 10.3390/molecules26164995
PMCID:
PMC8401439
AbstractArticlePDF–54M
15.
Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity
Zaibo Yang, Pei Li, Xiuhai Gan
Molecules. 2018 Jul; 23(7): 1798. Published online 2018 Jul 20. doi: 10.3390/molecules23071798
PMCID:
PMC6100116
AbstractArticlePDF–419K
16.
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro
Kareem A. Galal, Anna Truong, Frank Kwarcinski, Chandi de Silva, Krisha Avalani, Tammy M. Havener, Michael E. Chirgwin, Eric Merten, Han Wee Ong, Caleb Willis, Ahmad Abdelwaly, Mohamed A. Helal, Emily R. Derbyshire, Reena Zutshi, David H. Drewry
J Med Chem. 2022 Oct 13; 65(19): 13172–13197. Published online 2022 Sep 27. doi: 10.1021/acs.jmedchem.2c00996
PMCID:
PMC9574854
AbstractArticlePDF–5.0M
17.
Synthesis and in vitro evaluation of benzo[b]thiophene-3-carboxylic acid 1,1-dioxide derivatives as anticancer agents targeting the RhoA/ROCK pathway
Jinhao Liang, Jin Huang, Jianzhan Yang, Weihong Liang, Haoxiang Li, Yunshan Wu, Bo Liu
J Enzyme Inhib Med Chem. 2024; 39(1): 2390911. Published online 2024 Sep 11. doi: 10.1080/14756366.2024.2390911
PMCID:
PMC11391881
AbstractArticlePDF–2.2M
18.
Novel Indole-Pyrazole Hybrids as Potential Tubulin-Targeting Agents; Synthesis, antiproliferative evaluation, and molecular modeling studies
Mohammed Hawash, Sezen Guntekin Ergun, Deniz Cansen Kahraman, Abdurrahman Olgac, Ernest Hamel, Rengul Cetin-Atalay, Sultan Nacak Baytas
J Mol Struct. Author manuscript; available in PMC 2024 Aug 5.
Published in final edited form as: J Mol Struct. 2023 Aug 5; 1285: 135477. Published online 2023 Mar 31. doi: 10.1016/j.molstruc.2023.135477
PMCID:
PMC10208593
AbstractArticlePDF–2.6M
19.
Structure–Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D
Elliot D. Mock, Ioli Kotsogianni, Wouter P. F. Driever, Carmen S. Fonseca, Jelle M. Vooijs, Hans den Dulk, Constant A. A. van Boeckel, Mario van der Stelt
J Med Chem. 2021 Jan 14; 64(1): 481–515. Published online 2020 Dec 31. doi: 10.1021/acs.jmedchem.0c01441
PMCID:
PMC7816197
AbstractArticlePDF–3.2M
20.
An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety
Renzo Rossi, Maurizio Ciofalo
Molecules. 2020 Nov; 25(21): 5133. Published online 2020 Nov 4. doi: 10.3390/molecules25215133
PMCID:
PMC7663458
AbstractArticlePDF–19M

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