Mahboobi, Siavosh and Popp, Alfred and Fleck, W. F. (1999) Synthesis and biological evaluation of 4,4-dimethyl-5,5-di(1-methylethyl)-2,3,4,5-tetrahydro-l H-dipyrrolo[3,4-d : 2,1-f][1,2]azasiline-1,3-dione and other pyrrolediones as new antibacterial active agents. PHARMAZIE, 54 (10). pp. 730-733. ISSN 0031-7144,
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The UV-light induced photosubstitution of 3,4-dibromo-2,5-dihydro-1H-2,5-pyrroledione (2) [1] with pyrrole derivatives leads to 3-mono- and 3,4-disubstituted pyrrolediones depending on the starting material. These pyrrole homologues of arcyriarubin A (1) are further processed by nucleophilic substitution of the remaining bromine substituent with pyrrolidine. Cleavage of the protecting group affords the free pyrrole substituents. By UV-light irradiation the azasiline-system (6) is accessible, and its structure was established by X-ray methods. The in vitro antibacterial activity of the pyrrolediones was evaluated, and a strong activity of the compounds 4, 7, 8 and 12 against the methicillin- and ciprofloxacin-resistant bacterium Staphylococcus aureus 134/94 was established.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PROTEIN-KINASE-C; INHIBITORS; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 20 Dec 2022 16:06 |
| Last Modified: | 20 Dec 2022 16:06 |
| URI: | https://pred.uni-regensburg.de/id/eprint/48974 |
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