《Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5》 was written by Ortiz Zacarias, Natalia V.; van Veldhoven, Jacobus P. D.; den Hollander, Lisa S.; Dogan, Burak; Openy, Joseph; Hsiao, Ya-Yun; Lenselink, Eelke B.; Heitman, Laura H.; IJzerman, Adriaan P.. Related Products of 4949-44-4This research focused ontriazolopyrimidinone preparation chemokine receptor antagonist. The article conveys some information:
In this study, synthesis and the biol. activity of a series of triazolopyrimidinones I (R1 = Ph, 2-MeOC6H4, 3-ClC6H4, 3,4-Cl2C6H3, etc.; R2 = H, Me, H2N; R3 = Me, Et, i-Pr, cyclopropyl, Ph, etc.) as intracellular antagonists for CC chemokine receptors 2 and 5 (CCR2 and CCR5) are reported. Radioligand binding assays first showed that these compounds bind to the intracellular site of CCR2, and in combination with functional assays on CCR5, structure-affinity/activity relationships in both receptors were explored. Although most compounds were CCR2-selective, the compounds I (R1 = 2,3-Cl2C6H3, 3-Br-4-ClC6H3; R2 = H2N; R3 = i-Pr) inhibited β-arrestin recruitment in CCR5 with high potency. Moreover, these compounds displayed an insurmountable mechanism of inhibition in both receptors, which holds promise for improved efficacy in inflammatory diseases.Ethyl 3-oxopentanoate(cas: 4949-44-4Related Products of 4949-44-4) was used in this study.
Ethyl 3-oxopentanoate(cas: 4949-44-4) belongs to ketone compounds. They are most widely used as solvents, especially in industries manufacturing explosives, lacquers, paints, and textiles. Ketones are also used in tanning, as preservatives, and in hydraulic fluids.Related Products of 4949-44-4
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