30011-36-0Relevant articles and documents
Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators
Kong, Xue-Qing,Wei, Bing-Yan,Yu, Chen-Xi,Guan, Xiang-Na,Ma, Wei-Ping,Liu, Gang,Yang, Cai-Guang,Nan, Fa-Jun
supporting information, p. 1111 - 1115 (2020/07/06)
To combat multidrug-resistant Gram-positive bacteria, new antimicrobials particularly those with novel mechanism of action are badly needed. Different with conventional antibiotics which are typical inhibitors, small-molecule activators of bacterial ClpP represent a new class of antibiotics. No ClpP activator has been developed for clinical trial. Herein, we conducted a screening on our library of bengamide-like ring-opened analogues and found that L472-2 possesses a low minimum inhibitory concentration (MIC) against S.aureus and shows no activity for ClpP activation in vitro, but it displayed reduced antibacterial activity against S. aureus with clpP deletion. In order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity, we perform further structural modifications starting from L472-2. Compound 37 remains the antimicrobial activity and activation of ClpP protein in vitro, which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.
Silver-Catalyzed Cyclization of Propargylic Amides to Oxazolines
Wong, Valerie H. L.,White, Andrew J. P.,Hor,Hii
supporting information, p. 3943 - 3948 (2016/01/25)
A ligand-accelerated effect is observed in the cyclization of propargylic amides catalyzed by bis(pyridyl)silver(I) complexes, with an unexpected reversal of electronic demand to the analogous NH addition reaction. The catalyst was found to be effective for internal alkyne substrates, offering exclusive selectivity for the 5-exo-dig product. Differences in selectivity profile between gold- and silver-catalyzed processes are highlighted and discussed.
N-Triphenylphosphorylidene-1-(benzotriazol-1-yl)methylamine, a Novel Synthon Equivalent to +CH2NH2: The Preparation of Primary Amines
Katritzky, Alan R.,Jiang, Jinlong,Urogdi, Laszlo
, p. 3303 - 3306 (2007/10/02)
Primary amines are readily prepared by reaction of the title compound with organolithiums or Grignard reagents.