75759-65-8Relevant academic research and scientific papers
Synthesis and structure-activity relationship of uracil nucleotide derivatives towards the identification of human P2Y6 receptor antagonists
Meltzer, Diana,Ethan, Ophir,Arguin, Guillaume,Nadel, Yael,Danino, Ortal,Lecka, Joanna,Sévigny, Jean,Gendron, Fernand-Pierre,Fischer, Bilha
supporting information, p. 5764 - 5773 (2015/11/11)
P2Y6 receptor (P2Y6-R) is involved in various physiological and pathophysiological events. With a view to set rules for the design of UDP-based reversible P2Y6-R antagonists as potential drugs, we established structure-activity relationship of UDP analogues, bearing modifications at the uracil ring, ribose moiety, and the phosphate chain. For instance, C5-phenyl- or 3-NMe-uridine-5′-α,β-methylene-diphosphonate, 16 and 23, or lack of 2′-OH, in 12-15, resulted in loss of both agonist and antagonist activity toward hP2Y6-R. However, uridylyl phosphosulfate, 19, selectively inhibited hP2Y6-R (IC50 112 μM) versus P2Y2/4-Rs. In summary, we have established a comprehensive SAR for hP2Y6-R ligands towards the development of hP2Y6-R antagonists.
A SIMPLE SYNTHESIS OF FLUORESCENT URIDINES BY PHOTOCHEMICAL METHOD
Saito, Isao,Ito, Satoru,Shinmura, Tetsuya,Matsuura, Teruo
, p. 2813 - 2816 (2007/10/02)
A strongly fluorescent 5-pyrenyluridine was prepared by the photoreaction of 2',3'-O-isopropylidene-5-iodouridine with pyrene.Several fluorescent analogues of uracil were synthesized by similar procedures.
