163706-61-4Relevant articles and documents
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.
Synthesis of AZT 5′-triphosphate mimics and their inhibitory effects on HIV-1 reverse transcriptase
Wang, Guangyi,Boyle, Nicholas,Chen, Fu,Rajappan, Vasanthakumar,Fagan, Patrick,Brooks, Jennifer L.,Hurd, Tiffany,Leeds, Janet M.,Rajwanshi, Vivek K.,Jin, Yi,Prhavc, Marija,Bruice, Thomas W.,Dan Cook
, p. 6902 - 6913 (2007/10/03)
In search of active nucleoside 5′-triphosphate mimics, we have synthesized a series of AZT triphosphate mimics (AZT P3Ms) and evaluated their inhibitory effects on HIV-1 reverse transcriptase as well as their stability in fetal calf serum and in CEM cell
Process for preparing methylene bisphosphonic and salts
-
Page column 3-4, (2010/11/30)
A process for the preparation of salts of substituted or unsubstituted methylene bisphosphonic acids by hydrolysing the corresponding acid ester with hydrochloric acid, removing water from the acid azeotropically prior to addition of an amine or a base to