- Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors
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A series of UTP, UDP, and UMP derivatives and analogues were synthesized and evaluated at the human pyrimidinergic P2Y receptor subtypes P2Y2, P2Y4, and P2Y6 stably expressed in 1321N1 astrocytoma cells. Substituents at N3
- El-Tayeb, Ali,Qi, Aidong,Müller, Christa E.
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p. 7076 - 7087
(2007/10/03)
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- Azines and azoles. CXX. Synthesis of acyclic analogs of N 1-ribosides of barbituric acid and its 5-ylidene derivatives
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The reaction of 2,4,6-tris(trimethylsiloxy)pyrimidine with 2-oxabutane-1,4-diyl diacetate in methylene chloride in methylene chloride in the presence of SnCl4 proceeds regioselectively to form 1-[(2-acetoxyethoxy)methyl]barbituric acid. The latter is readily deacetylated to a free acyclic analog of N-ribosides of barbituric acid. 1-[(2-Acetoxy- and 2-hydroxyethoxy)methyl]barbituric acids easily react with aromatic and heterocyclic aldehydes in water and organic solvents, forming 5-ylidenebarbituric acids. The structure of the products was proved by 1H NMR and UV spectroscopy. Certain of the products exhibit a moderate antimicrobial and antiviral activity.
- Studentsov,Kokhanovskii,Ganina,Nikolaeva,Fedorova,Moskvin,Ivin
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p. 261 - 265
(2007/10/03)
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- AZINES AND AZOLES. LXXXIX. SYNTHESIS AND STRUCTURE OF RIBOSYLATED BARBITURIC ACIDS
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Ribosylation of barbituric acid according to the silyl version of the Hilbert-Johnson method yields a mixture of 1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)barbituric acid and 1,3-bis(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)barbituric acid.These were separated and converted into the deacetylated analogs.The structure of the obtained compounds is discussed on the basis of their IR, 1H and 13C NMR, CD, and UV spectra.
- Moskvin, A. V.,Ksenofontova, G. V.,Studentsov, E. P.,Ivin, B. A.
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p. 440 - 446
(2007/10/02)
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- Synthesis of a New Class of Uridine Phoshorylase Inhibitors
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A new series of potent uridine phosphorylase inhibitors have been prepared from barbituric acid.Among them 1--5-(m-benzyloxy)benzylbarbituric acid (37, BBBA) is the most promising having a Ki value of 1.1 +/- 0.2 nM wit
- Tzeng, Cherng-Chyi,Panzica, Raymond P.,Naguib, Fardos N.M.,Kouni, Mahmoud H. el
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p. 1399 - 1404
(2007/10/02)
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