35051-49-1Relevant articles and documents
Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives against Gram-Negative Multidrug-Resistant Pathogens
Kong, Qidi,Pan, Wei,Xu, Heng,Xue, Yaru,Guo, Bin,Meng, Xin,Luo, Cheng,Wang, Ting,Zhang, Shuhua,Yang, Yushe
supporting information, p. 8644 - 8665 (2021/06/28)
Due to the poor permeability across Gram-negative bacterial membranes and the troublesome bacterial efflux mechanism, only a few GyrB/ParE inhibitors with potent activity against Gram-negative pathogens have been reported. Among them, pyrimido[4,5-b]indol
Synthesis and characterization of novel phosphonocarboxylate inhibitors of RGGT
Coxon, Fraser,Joachimiak, ?ukasz,Najumudeen, Arafath Kaja,Breen, George,Gmach, Joanna,Oetken-Lindholm, Christina,Way, Rebecca,Dunford, James,Abankwa, Daniel,B?azewska, Katarzyna M.
supporting information, p. 77 - 89 (2014/07/22)
Phosphonocarboxylate (PC) analogs of the anti-osteoporotic drugs, bisphosphonates, represent the first class of selective inhibitors of Rab geranylgeranyl transferase (RabGGTase, RGGT), an enzyme implicated in several diseases including ovarian, breast and skin cancer. Here we present the synthesis and biological characterization of an extended set of this class of compounds, including lipophilic derivatives of the known RGGT inhibitors. From this new panel of PCs, we have identified an inhibitor of RGGT that is of similar potency as the most active published phosphonocarboxylate, but of higher selectivity towards prenyl pyrophosphate synthases. New insights into structural requirements are also presented, showing that only PC analogs of the most potent 3rd generation bisphosphonates inhibit RGGT. In addition, the first phosphonocarboxylate-derived GGPPS weak inhibitor is reported.
Microwave-assisted alkylation of diethyl ethoxycarbonylmethylphosphonate under solventless conditions
Gruen, Alajos,Blastik, Zsofia,Drahos, Laszlo,Keglevich, Gyoergy
experimental part, p. 241 - 246 (2012/07/28)
The reaction of diethyl ethoxycarbonylmethylphosphonate with a series of alkyl halides, under microwave (MW) and solventless conditions at 120°C, in the presence of Cs2CO3 and in the absence of a phase transfer catalyst afforded the corresponding monoalkylated products in yields of >70%. The thermal variant carried out in boiling acetonitrile was slow and led to incomplete conversions. In the MW method, the phase transfer catalyst is substituted by MW irradiation and there is no need for a solvent.
