Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships

A series of fluoroquinolone antibacterials having the 7-position (10-position of pyridobenzoxazines) substituted with 2,7-diazaspiro[4.4]nonane (4b), 1,7-diazaspiro[4.4]nonane (5a), or 2,8-diazaspiro[5.5]undecane (6b) was prepared, and their biological activities were compared with piperazine and py...

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Veröffentlicht in:	Journal of medicinal chemistry 1990-08, Vol.33 (8), p.2270-2275
Hauptverfasser:	Culbertson, Townley P, Sanchez, Joseph P, Gambino, Laura, Sesnie, Josephine A
Format:	Artikel
Sprache:	eng
Schlagworte:	Bacteria - drug effects Chemical Phenomena Chemistry Exact sciences and technology Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Molecular Structure Organic chemistry Piperazines - pharmacology Preparations and properties Pyrrolidines - pharmacology Quinolines - chemical synthesis Quinolines - pharmacology Spiro Compounds - chemical synthesis Spiro Compounds - pharmacology Structure-Activity Relationship
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Zusammenfassung:	A series of fluoroquinolone antibacterials having the 7-position (10-position of pyridobenzoxazines) substituted with 2,7-diazaspiro[4.4]nonane (4b), 1,7-diazaspiro[4.4]nonane (5a), or 2,8-diazaspiro[5.5]undecane (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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00170a035