425-75-2Relevant articles and documents
Synthesis and bioactivity investigation of quinone-based dimeric cationic triazolium amphiphiles selective against resistant fungal and bacterial pathogens
Shrestha, Jaya P.,Baker, Coleman,Kawasaki, Yukie,Subedi, Yagya P.,Vincent de Paul, Nzuwah Nziko,Takemoto, Jon Y.,Chang, Cheng-Wei Tom
, p. 1 - 17 (2017)
A series of synthetic dimeric cationic anthraquinone analogs (CAAs) with potent antimicrobial activities against a broad range of fungi and bacteria were developed. These compounds were prepared in 2–3 steps with high overall yield and possess alkyl chain, azole, quinone, and quaternary ammonium complexes (QACs). In vitro biological evaluations reveal prominent inhibitory activities of lead compounds against several drug-susceptible and drug-resistant fungal and bacterial strains, including MRSA, VRE, Candida albicans and Aspergillus flavus. Mode of action investigation reveals that the synthesized dimeric CAA's can disrupt the membrane integrity of fungi. Computational studies reveal possible designs that can revive the activity of QACs against drug-resistant bacteria. Cytotoxicity assays in SKOV-3, a cancer cell line, show that the lead compounds are selectively toxic to fungi and bacteria over human cells.
Lysine Ethylation by Histone Lysine Methyltransferases
Al Temimi, Abbas H. K.,Martin, Michael,Meng, Qingxi,Lenstra, Danny C.,Qian, Ping,Guo, Hong,Weinhold, Elmar,Mecinovi?, Jasmin
, p. 392 - 400 (2019/11/13)
Biomedicinally important histone lysine methyltransferases (KMTs) catalyze the transfer of a methyl group from S-adenosylmethionine (AdoMet) cosubstrate to lysine residues in histones and other proteins. Herein, experimental and computational investigations on human KMT-catalyzed ethylation of histone peptides by using S-adenosylethionine (AdoEth) and Se-adenosylselenoethionine (AdoSeEth) cosubstrates are reported. MALDI-TOF MS experiments reveal that, unlike monomethyltransferases SETD7 and SETD8, methyltransferases G9a and G9a-like protein (GLP) do have the capacity to ethylate lysine residues in histone peptides, and that cosubstrates follow the efficiency trend AdoMet>AdoSeEth>AdoEth. G9a and GLP can also catalyze AdoSeEth-mediated ethylation of ornithine and produce histone peptides bearing lysine residues with different alkyl groups, such as H3K9meet and H3K9me2et. Molecular dynamics and free energy simulations based on quantum mechanics/molecular mechanics potential supported the experimental findings by providing an insight into the geometry and energetics of the enzymatic methyl/ethyl transfer process.
A continuous preparation method of triflic acid ethyl ester
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Paragraph 0018; 0019, (2017/02/09)
A disclosed method for continuously preparing ethyl trifluoromethanesulfonate comprises the following steps: (1) adding trifluoromethanesulfonic acid and diethyl sulfate with the molar ratio of (1-2):1 into a reaction kettle, switching on a stirring apparatus, raising the temperature of the reaction kettle to 50-100 DEG C, and keeping the temperature for reacting for 2-6 h; and (2) raising the temperature of the reaction kettle to 100-150 DEG C, switching on a rectifying apparatus, controlling the reflux ratio of the rectifying apparatus at (1-3):(3-1), continuously introducing trifluoromethanesulfonic acid and diethyl sulfate into the reaction kettle, controlling the speed of trifluoromethanesulfonic acid introduced into the reaction kettle at 30-70 g/min, controlling the speed of diethyl sulfate introduced into the reaction kettle at 10-50 g/min, and collecting a distillation fraction and condensing to obtain ethyl trifluoromethanesulfonate. The preparation method is short in production period and low in energy consumption, and prepared ethyl trifluoromethanesulfonate has the purity larger than 99%, the yield is 90% or more, and industrialized production can be realized.
