52888-70-7Relevant academic research and scientific papers
Synthesis method of succinic acid derivative or 3 -arylpropionic acid (by machine translation)
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Paragraph 0101-0114; 0115; 0132, (2020/10/30)
The invention discloses a synthesis method of a succinic acid derivative or 3 -arylpropionic acid, which comprises the following steps: adding a base in a drying reaction tube and CO removing CO. 2 The reaction is carried out under the irradiation of visible light, the reaction is carried out under visible light irradiation, and then separation and purification are carried out to obtain the butanedioic acid derivative or 3 -arylpropionic acid product; the base comprises sodium tert-butoxide, potassium tert-butoxide, lithium tert-butyl alcohol and 4 - potassium carbonate; and the reaction substrate comprises an acrylate compound or an aryl vinyl compound. CO can be induced by visible light. 2 The scheme provided by the invention is mild in reaction condition and wide in reaction 3 - substrate selectivity, and the reaction substrate is wide in selectivity, the raw materials are cheap and easily available, and the method has a good industrial application prospect. (by machine translation)
Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents
Yang, Yinghong,Wang, Zhenling,Yang, Jianzhong,Yang, Tao,Pi, Weiyi,Ang, Wei,Lin, Yanni,Liu, Yuanyuan,Li, Zicheng,Luo, Youfu,Wei, Yuquan
, p. 954 - 957 (2012/03/11)
A series of compounds with a diphenyl ether nucleus were synthesized by incorporating various amines into the diphenyl ether scaffold with an amide bond. Their antitubercular activities were evaluated against Mycobacterium tuberculosis H37Rv by a microdilution method, with MIC values ranging from 4 to 64 μg/mL. Through structure-activity relationship studies, the two chlorine atoms at 3 and 4 positions in the phenyl ring of R2 group were found to play a significant role in the antitubercular activity. The most potent compound 6c showed an MIC value of 4 μg/mL and a good safety profile in HepG2 cell line by the MTT assay. Compound 6c was further found to be effective in a murine model of BCG infection, providing a good lead for subsequent optimization.
PHENYLALKYLCARBOXYLIC ACID DELIVERY AGENTS
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Page/Page column 34, (2008/12/07)
The present invention provides phenylalkylcarboxylic acid compounds and compositions containing such compounds which facilitate the delivery of biologically active agents.
Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: Pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea
Adams, Jerry L.,Garigipati, Ravi S.,Sorenson, Margaret,Schmidt, Stanley J.,Brian, William R.,Newton, John F.,Tyrrell, Kathy A.,Garver, Eric,Yodis, Lee A.,Chabot-Fletcher, Marie,Tzimas, Maritsa,Webb, Edward F.,Breton, John J.,Griswold, Don E.
, p. 5035 - 5046 (2007/10/03)
A series of N-hydroxyurea derivatives have been prepared and examined as inhibitors of 5-lipoxygenase. Oral activity was established by examining the inhibition of LTB4 biosynthesis in an ex vivo assay in the mouse. The pharmacodynamic performance in the mouse of selected compounds was assessed using an ex vivo LTB4 assay and an adoptive peritoneal anaphylaxis assay at extended pretreat times. Compounds with an extended duration of action were reexamined as the individual enantiomers in the ex vivo assay, and the (S) enantiomer of N-hydroxy-N-[2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl]urea, (+)-1a (SB 202235), was selected as the compound with the best overall profile. Higher plasma concentrations and longer plasma half-lives were found for (+)-1a relative to its enantiomer in the mouse, monkey, and dog. In vitro metabolic studies in mouse liver microsomes established enantiospecific glucuronidation as a likely mechanism for the observed differences between the enantiomers of 1a. Enantioselective glucuronidation favoring (-)-1a was also found in human liver microsomes.
