So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Wu, Peng; Bjoern-Yoshimoto, Walden E.; Staudt, Markus; Jensen, Anders A.; Bunch, Lennart researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Synthetic Route of C4H5N3.They published the article 《Identification and Structure-Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3)》 about this compound( cas:591-54-8 ) in ACS Chemical Neuroscience. Keywords: imidazopyridineamine preparation inhibitor excitatory amino acid transporter subtype EAAT3; EAAT3; EAAT3 inhibitors; Glutamate; excitatory amino acid transporter. We’ll tell you more about this compound (cas:591-54-8).
Screening of a library of 49,087 compounds at the excitatory amino acid transporter subtype 3 (EAAT3) led to the identification of 2-(furan-2-yl)-8-methyl-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine which showed a >20-fold preference for inhibition of EAAT3 (IC50 = 13 μM) over EAAT1,2,4 (EAAT1: IC50 ∼ 250 μM; EAAT2,4: IC50 > 250 μM). A small lipophilic substituent (Me or bromine) at the 7- and/or 8-position was essential for activity. Furthermore, the substitution pattern of the o-tolyl group (compound I) and the chem. nature of the substituent in the 2-position of tert-Bu 3-(8-bromo-7-methyl-3-(o-tolylamino)imidazo[1,2-a]pyridin-2-yl)azetidine-1-carboxylate are essential for the selectivity toward EAAT3 over EAAT1,2. The most prominent analogs to come out of this study are 2-(furan-2-yl)-8-methyl-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine and 8-Bromo-2-(furan-2-yl)-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine that display ∼35-fold selectivity for EAAT3 (IC50 = 7.2 μM) over EAAT1,2,4 (IC50 ∼ 250 μM).
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