478912-40-2Relevant academic research and scientific papers
Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
Yang, Shouning,Shi, Wei,Xing, Dong,Zhao, Zheng,Lv, Fengping,Yang, Liping,Yang, Yushe,Hu, Wenhao
, p. 133 - 152 (2014/10/15)
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.
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors
Shi, Wei,Duan, Yuejiao,Qian, Yu,Li, Ming,Yang, Liping,Hu, Wenhao
scheme or table, p. 3592 - 3595 (2010/09/06)
The synthesis and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated, and some of these derivatives showed better in vitro antibacterial activity than existing drugs, including penicillin, ciprofloxacin, vancomycin, and linezolid.
N-FORMYL HYDROZYAMINE COMPOUNDS
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Page/Page column 7-8, (2009/04/24)
Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compou
Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results
Pichota, Arkadius,Duraiswamy, Jeyaraj,Yin, Zheng,Keller, Thomas H.,Alam, Jenefer,Liung, Sarah,Lee, Gladys,Ding, Mei,Wang, Gang,Chan, Wai Ling,Schreiber, Mark,Ma, Ida,Beer, David,Ngew, Xinyi,Mukherjee, Kakoli,Nanjundappa, Mahesh,Teo, Jeanette W.P.,Thayalan, Pamela,Yap, Amelia,Dick, Thomas,Meng, Wuyi,Xu, Mei,Koehn, James,Pan, Shi-Hao,Clark, Kirk,Xie, Xiaoling,Shoen, Carolyn,Cynamon, Michael
scheme or table, p. 6568 - 6572 (2009/09/30)
Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of highly potent inhibitors of Mycobacterium tuberculosis (Mtb) PDF enzyme as well as the first X-ray crystal structure of Mtb PDF. Structure-activity relationship and crystallographic data clarified the structural requirements for high enzyme potency and cell based potency. Activities against single and multi-drug-resistant Mtb strains are also reported.
PDF INHIBITORS
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, (2010/11/28)
The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.
A practical enantioselective synthesis of a novel peptide deformylase inhibitor
Slade, Joel,Parker, David,Girgis, Michael,Mueller, Martin,Vivelo, James,Liu, Hui,Bajwa, Joginder,Chen, Guang-Pei,Carosi, Joseph,Lee, Paul,Chaudhary, Apurva,Wambser, Dana,Prasad, Kapa,Bracken, Kathryn,Dean, Karl,Boehnke, Helmut,Repic, Oljan,Blacklock, Thomas J.
, p. 78 - 93 (2012/12/21)
A practical synthesis of the peptide deformylase inhibitor LBM415,(2S)-N-(5-fluoro-1-oxido-2-pyridinyl)-1-[(2R)-2-[(formylhydroxyamino) methyl]-1-oxohexyl]-2-pyrrolidinecarboxamide, magnesium salt 11, is described. The key chiral intermediate, (2S)-N-(5-f
N-FORMYL HYDROXYLAMINE COMPOUNDS
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Page/Page column 18-19, (2008/06/13)
Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compou
