- Quinolone Antibacterial Agents Substituted at the 7-Position with Spiroamines. Synthesis and Structure-Activity Relationships
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A series of fluoroquinolone antibacterials having the 7-position (10-position of pyridobenzoxazines) substituted with 2,7-diazaspirononane (4b), 1,7-diazaspirononane (5a), or 2,8-diazaspiroundecane (6b) was prepared, and their biological activities were compared with piperazine and pyrrolidine substituted analogues.Most exhibited potent Gram-positive and Gram-negative activity, especially when side chain 4b was N-alkylated.
- Culbertson, Townley P.,Sanchez, Joseph P.,Gambino, Laura,Sesnie, Josephine A.
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p. 2270 - 2275
(2007/10/02)
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- SYNTHESIS AND ABSOLUTE CONFIGURATION OF THREE ISOMERIC SPIRO-BIS(2-PYRROLIDINONES)
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Syntheses are described for three isomeric spiro-bis-(2-pyrrolidinones): 2,7-diazaspirononane-3,8-dione (II), 2,7-diazaspirononane-1,8-dione (IV) and 1,7-diazaspirononane-2,8-dione (VI).All the syntheses were carried out starting from 3-carboxy-5-oxo-3-pyrrolidineacetic acid (VIII) of known configuration, allowing the assignation of absolute configuration to compounds II, IV and VI synthetized through stereochemically unequivocal reaction steps.
- Kajtar, Marton,Hollosi, Miklos,Kinsky, Klaus,Majer, Zsuzsanna
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p. 936 - 949
(2007/10/02)
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