Synthesis and structural–activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents
The synthesis and SAR of the 3-hydroxyquinazoline diones, a novel class of bacterial topoisomerase inhibitors, is reported. A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4405-4409 |
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| container_issue | 17 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 14 |
| creator | Tran, Tuan P. Ellsworth, Edmund L. Stier, Michael A. Domagala, John M. Hollis Showalter, H.D. Gracheck, Stephen J. Shapiro, Martin A. Joannides, Themis E. Singh, Rajeshwar |
| description | The synthesis and SAR of the 3-hydroxyquinazoline diones, a novel class of bacterial topoisomerase inhibitors, is reported.
A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against
E. coli gyrase and significant in vitro Gram-negative and Gram-positive antibacterial activity. |
| doi_str_mv | 10.1016/j.bmcl.2004.06.063 |
| format | Article |
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A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against
E. coli gyrase and significant in vitro Gram-negative and Gram-positive antibacterial activity.</description><subject>3-Hydroxyquinazoline-2,4-diones</subject><subject>Anti-Bacterial Agents - chemical synthesis</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Bacterial topoisomerase inhibitors</subject><subject>Biological and medical sciences</subject><subject>Hydroxyquinolines - chemical synthesis</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests - statistics & numerical data</subject><subject>Miscellaneous</subject><subject>Pharmacology. 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A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against
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| ispartof | Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (17), p.4405-4409 |
| issn | 0960-894X 1464-3405 |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | 3-Hydroxyquinazoline-2,4-diones Anti-Bacterial Agents - chemical synthesis Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacterial topoisomerase inhibitors Biological and medical sciences Hydroxyquinolines - chemical synthesis Medical sciences Microbial Sensitivity Tests - statistics & numerical data Miscellaneous Pharmacology. Drug treatments Quinazolines - chemical synthesis Structure-Activity Relationship |
| title | Synthesis and structural–activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents |
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