Small Antimicrobial Agents Based on Acylated Reduced Amide Scaffold
Document Type
Article
Publication Date
2016
Digital Object Identifier (DOI)
https://doi.org/10.1021/acs.jmedchem.6b00640
Abstract
Prevalence of drug-resistant bacteria has emerged to be one of the greatest threats in the 21st century. Herein, we report the development of a series of small molecular antibacterial agents that are based on the acylated reduced amide scaffold. These molecules display good potency against a panel of multidrug-resistant Gram-positive and Gram-negative bacterial strains. Meanwhile, they also effectively inhibit the biofilm formation. Mechanistic studies suggest that these compounds kill bacteria by compromising bacterial membranes, a mechanism analogous to that of host-defense peptides (HDPs). The mechanism is further supported by the fact that the lead compounds do not induce resistance in MRSA bacteria even after 14 passages. Lastly, we also demonstrate that these molecules have therapeutic potential by preventing inflammation caused by MRSA induced pneumonia in a rat model. This class of compounds could lead to an appealing class of antibiotic agents combating drug-resistant bacterial strains.
Was this content written or created while at USF?
Yes
Citation / Publisher Attribution
Journal of Medicinal Chemistry, v. 59, issue 17, p. 7877-7887
Scholar Commons Citation
Teng, Peng; Huo, Da; Nimmagadda, Alekhya; Wu, Jianfeng; She, Fengyu; Su, Ma; Lin, Xiaoyang; Yan, Jiyu; Cao, Annie; Xi, Chuanwu; Hu, Yong; and Cai, Jianfeng, "Small Antimicrobial Agents Based on Acylated Reduced Amide Scaffold" (2016). Chemistry Faculty Publications. 191.
https://digitalcommons.usf.edu/chm_facpub/191
