Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ
| Autor: | Jared T. Moore, Valerie Huynh, Kevin S. Martin, Terrence E. O’Brien, Zi Yao, David E. Anderson, James B. Ames, Clarissa Tadeus, Luiz A. E. Pollo, Gabriella M. Nepomuceno, Katie M. Chan, Jared T. Shaw, Francisco J. Sarabia |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
bacterial cell division
macromolecular substances GTPase medicine.disease_cause FtsZ physiological processes Biochemistry Bacterial cell structure Medicinal and Biomolecular Chemistry Drug Discovery medicine Escherichia coli Molecular interactions biology Organic Chemistry Pharmacology and Pharmaceutical Sciences Cell biology Emerging Infectious Diseases 5.1 Pharmaceuticals biology.protein zantrin Z3 bacteria biological phenomena cell phenomena and immunity SAR |
| Zdroj: | Nepomuceno, GM; Chan, KM; Huynh, V; Martin, KS; Moore, JT; Obrien, TE; et al.(2015). Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ. ACS Medicinal Chemistry Letters, 6(3), 308-312. doi: 10.1021/ml500497s. UC Davis: Retrieved from: http://www.escholarship.org/uc/item/6098r49t ACS medicinal chemistry letters, vol 6, iss 3 |
| DOI: | 10.1021/ml500497s. |
| Popis: | © 2015 American Chemical Society. The bacterial cell division protein FtsZ is one of many potential targets for the development of novel antibiotics. Recently, zantrin Z3 was shown to be a cross-species inhibitor of FtsZ; however, its specific interactions with the protein are still unknown. Herein we report the synthesis of analogues that contain a more tractable core structure and an analogue with single-digit micromolar inhibition of FtsZs GTPase activity, which represents the most potent inhibitor of Escherichia coli FtsZ reported to date. In addition, the zantrin Z3 core has been converted to two potential photo-cross-linking reagents for proteomic studies that could shed light on the molecular interactions between FtsZ and molecules related to zantrin Z3. |
| Databáze: | OpenAIRE |
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