Structure-based Discovery of Novel Antibacterials

ISSN: 2211-3533 (Online)
ISSN: 2211-3525 (Print)

Volume 14, 2 Issues, 2016

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Anti-Infective Agents

Formerly: Anti-Infective Agents in Medicinal Chemistry

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Structure-based Discovery of Novel Antibacterials

Anti-Infective Agents, 9(4): 168-179.

Author(s): Huan-Qiu Li, Peng-Cheng Lv, Lei Shi and Hai-Liang Zhu.

Affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.


An increasing fraction of bacterial isolates show reduced susceptibility to our most trusted antibiotics. In order to prevent this serious medical problem, the elaboration of new types of antibacterial agents or the expansion of bioactivity of the previous drugs is a very important task. Different targets in key areas of the bacterial cell cycle have been studied that would be a new weapon against this threat. In this review we attempt to summarize the recent progress made in the field of some represent bacterial enzyme inhibitors and the structure-based drug design of new broad-spectrum antibacterial agents. Based on the structure design and protein target, more and more novel compounds were discovered for the development of new antibacterial agents. It is expected that this review would serve as a stimulant for new thoughts in the quest for rational designs of more effective antibacterial drugs.The interaction of structure design with enzyme targets is fascinating, and this story is still unfolding for us to discover novel antibacterials.


Antibacterial, structure design, drug discovery, FabH, DNA gyrase A, DNA gyrase B, FtsZ, DdlB, VanA, Fluoroquinolones, protein target.

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Article Details

Volume: 9
Issue Number: 4
First Page: 168
Last Page: 179
Page Count: 12
DOI: 10.2174/187152110794785068
Price: $58
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