7-位被螺胺取代的喹诺酮类抗菌剂。合成及构效关系。

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

作者信息

Culbertson T P, Sanchez J P, Gambino L, Sesnie J A

机构信息

Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.

出版信息

J Med Chem. 1990 Aug;33(8):2270-5. doi: 10.1021/jm00170a035.

DOI:10.1021/jm00170a035

Abstract

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.

摘要

制备了一系列7位（吡啶并苯并恶嗪的10位）被2,7-二氮杂螺[4.4]壬烷（4b）、1,7-二氮杂螺[4.4]壬烷（5a）或2,8-二氮杂螺[5.5]十一烷（6b）取代的氟喹诺酮类抗菌剂，并将它们的生物活性与哌嗪和吡咯烷取代的类似物进行了比较。大多数表现出强效的革兰氏阳性和革兰氏阴性活性，尤其是当侧链4b被N-烷基化时。

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