Structure-based Discovery of Novel Antibacterials

Huan-Qiu      Li; Peng-Cheng      Lv; Lei      Shi; Hai-Liang      Zhu

Abstract

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.

Keywords: Antibacterial, structure design, drug discovery, FabH, DNA gyrase A, DNA gyrase B, FtsZ, DdlB, VanA.