Electric Literature of C12H14O3On May 25, 2018, Singh, L. Ravithej; Kumar, Ajeet; Upadhyay, Akanksha; Gupta, Sampa; Palanati, Gopala Reddy; Sikka, Kamakshi; Siddiqi, Mohammad Imran; Yadav, Prem N.; Sashidhara, Koneni V. published an article in European Journal of Medicinal Chemistry. The article was 《Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy》. The article mentions the following:
Rational designing and synthesis of coumarin-dihydroquinazolinone conjugates such as I [R1 = Me, i-Pr, s-Bu, etc.; R2 = H, 2-thienyl, 3,4-(MeO)2, etc.] to evaluate their agonist activity at GPR109a receptor was presented. Among the synthesized small mol. library, compound I [R1 = Me, R2 = 4-MeO] displayed robust agonist action at GPR109a with EC50 < 11nM. Homol. model of human GPR109a protein was generated to realize the binding interaction of the active mol. with the active site of GPR109a. Further, the efficacy of active compound I [R1 = Me, R2 = 4-MeO] was supported by in-vivo experiments which showed reduced body weight in diet induced obese mice model. Interestingly, compound I [R1 = Me, R2 = 4-MeO] reduced leptin in blood plasma and total serum cholesterol. These results suggested that the coumarin-dihydroquinazolinone conjugate is a suitable scaffold to further expand the chem. diversity and make them potential niacin receptor 1 agonist. After reading the article, we found that the author used 5-(tert-Butyl)-4-hydroxyisophthalaldehyde(cas: 153759-59-2Electric Literature of C12H14O3)
5-(tert-Butyl)-4-hydroxyisophthalaldehyde(cas: 153759-59-2) belongs to phenols.Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book).Electric Literature of C12H14O3
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