TY - JOUR
T1 - Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
AU - Yang, Shouning
AU - Shi, Wei
AU - Xing, Dong
AU - Zhao, Zheng
AU - Lv, Fengping
AU - Yang, Liping
AU - Yang, Yushe
AU - Hu, Wenhao
PY - 2014/10/30
Y1 - 2014/10/30
N2 - Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o′, 1q′, and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs.
AB - Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o′, 1q′, and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs.
KW - Drug resistant bacteria
KW - Peptide deformylase inhibitor
KW - Proline derivatives
UR - https://www.scopus.com/pages/publications/84906502930
U2 - 10.1016/j.ejmech.2014.07.106
DO - 10.1016/j.ejmech.2014.07.106
M3 - 文章
C2 - 25151577
AN - SCOPUS:84906502930
SN - 0223-5234
VL - 86
SP - 133
EP - 152
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -