876-02-8Relevant articles and documents
Preparation method for 4-methoxy-1,3-phthalic acid
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Paragraph 0039; 0040; 0041; 0042, (2017/12/04)
The invention provides a preparation method for 4-methoxy-1,3-phthalic acid. 4-methoxy-1,3-phthalic acid is key intermediate for preparation of an anti-platelet aggregation drug picotamide (with a trade name of plactidil). According to the preparation method, 4-methoxy-1,3-phthalic acid is prepared from the starting raw material p-methylphenol or o-methylphenol through esterification, Fries rearrangement, methylation, oxidation and acidification. Compared with traditional preparation methods, the preparation method provided by the invention has the advantages of low equipment investment, simple operation, quick reaction, high yield, low synthesis cost, greatly reduced environmental pollution and the like, and is particularly suitable for large-scale industrial production.
Investigation on the substitution effects of the flavonoids as potent anticancer agents: A structure-activity relationships study
Wang, Xiao-Bing,Yang, Lei,Kong, Ling-Yi,Liu, Wei,Guo, Qing-Long
, p. 1833 - 1849,17 (2020/07/30)
Three series of flavonoid analogues substituted with different aminomethyl substitutions at C-6, C-7, and C-8 were designed and synthesized for the structure-activity relationship studies as potent anticancer agents. The prepared analogues were evaluated for their in vitro inhibitory activity against the growth of the hepatic cancer cell lines HepG2 and SMMC-7721. Structure-activity relationships indicated that not only the compounds with amino methyl groups were more active than those without the groups in the same series but also the compounds substituted by aminomethyl groups at position C-8 were more active than those at positions C-6 and C-7.
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists
Makadia, Pankaj,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Patel, Darshit,Pola, Suresh,Thube, Baban,Priyadarshini, Priyanka,Suthar, Dinesh,Shah, Maanan,Giri, Suresh,Trivedi, Chitrang,Jain, Mukul,Patel, Pankaj,Bahekar, Rajesh
experimental part, p. 771 - 782 (2011/03/18)
A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARδ selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a, 12c, 17a and 18a showed PPAR-pan agonists activities and among these four compounds tested, 12a emerged as highly potent and efficacious compound, while 17a exhibited moderate and balanced PPAR-pan agonistic activity. In vivo, selected test compounds 12a and 17a exhibited significant anti-hyperglycemic and anti-hyperlipidemic activities in relevant animal models. These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists.
