- Quinolone Antibacterials: Preparation and Activity of Bridged Bicyclic Analogues of the C7-Piperazine
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A series of quinolone and naphthyridine antibacterial agents possessing as the C7-heterocycle bicyclic 2,5-diazabicycloalkanes, where n = 2, 3 and m = 1, 2, and a series including 4-aminopiperidine and 3-amino-8-azabicyclooctanes have been prepared and evaluated in vitro and in vivo for antibacterial activity against a variety of Gramm-negative and Gramm-positive organisms.These compounds were also tested against the target enzyme bacterial DNA gyrase.All the examples investigated are nearly equipotent with the parent 7-piperazinyl analogues.Only endo-7-(3-amino-8-azabicyclooct-8-yl) -1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid displays activity that surpasses that of the piperazine parent.
- Kiely, John S.,Hutt, Marland P.,Culbertson, Townley P.,Bucsh, Ruth A.,Worth, Donald F.,et al.
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p. 656 - 663
(2007/10/02)
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- Synthesis of Three pyridines
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The synthesis of o-, m, and p-pyridine by diborane/tetrahydrofuran reduction of the corresponding trifluoroacetamide is described.The yields were 52 percent, 83 percent, and 76 percent, respectively.The synthesis, in 53 percent yield, of 2,2,2-trifluoro-N-(4-pyridyl)acetamide is also described.
- Bissell, Eugene R.,Swansiger, Rosalind W.
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p. 234 - 235
(2007/10/02)
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