Synthesis and antibacterial activity of 7-hydrazinoquinolones

A series of new C-7 substituted hydrazino quinolones and naphthyridines were prepared and tested for antibacterial activity. The hydrazine bridge at the C-7 position did not favor the antibacterial activity, whereas the nature of other substituents at N-1, C-5 and C-8 did noticeably influence the an...

Full description

Saved in:
Bibliographic Details
Published in:European journal of medicinal chemistry 1998-09, Vol.33 (9), p.697-703
Main Authors: Singh, Rajeshwar, Fathi-Afshar, Rakhshandeh, Thomas, George, Singh, Maya Prakash, Higashitani, Fusahiro, Hyodo, Akio, Unemi, Norio, Micetich, Ronald George
Format: Article
Language:English
Subjects:
7-hydrazino substituted fluoroquinolones
antibacterial activity of fluoroquinolones
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
fluoroquinolone antibacterials
Medical sciences
Pharmacology. Drug treatments
structure-activity relationship of fluoroquinolone derivatives
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of new C-7 substituted hydrazino quinolones and naphthyridines were prepared and tested for antibacterial activity. The hydrazine bridge at the C-7 position did not favor the antibacterial activity, whereas the nature of other substituents at N-1, C-5 and C-8 did noticeably influence the antibacterial activity. The 7-(1-aminomorpholino) derivatives exhibited superior antibacterial activity against Gram-positive and inferior activity against Gram-negative bacteria than the 7-(1-aminopiperazinyl) derivatives. Substitution of the quinolone at position-1 with cyclopropyl was the most beneficial for antibacterial activity among the series of compounds prepared.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(98)80028-7