13345-08-9Relevant articles and documents
Synthesis of new series of pyrimido[4,5-b][1,4] benzothiazines as 15-lipoxygenase inhibitors and study of their inhibitory mechanism
Nikpour, Mohsen,Mousavian, Mina,Davoodnejad, Mahdieh,Alimardani, Maliheh,Sadeghian, Hamid
, p. 5036 - 5043 (2013/09/23)
A series of 2-substituted 4-n-propyl pyrimido[4,5-b][1,4]benzothiazines were synthesized, and evaluated as soybean 15-lipoxygenase (SLO) inhibitors. Among the synthesized compounds, 2-(4-methyl piperazinyl) analog showed the best SLO inhibition activity (IC50 = 8.9 ± 0.4 μM). To rationalize the inhibitory potency variation of the compounds, computer-assisted modeling of the enzyme-inhibitor, radical scavenging evaluation, and inhibitory mechanism analyses were performed. The results showed that in 4-alkyl pyrimido[4,5-b]benzothiazines with same 2-substituent, radical scavenging potency plays a key role in lipoxygenase inhibition.
Synthesis of modified uracil and cytosine nucleobases using a microwave-assisted method
Burgula, Laxmi Narayana,Radhakrishnan,Kundu, Lal Mohan
supporting information; experimental part, p. 2639 - 2642 (2012/06/30)
Modified nucleobases and nucleic acids have found many biological and pharmaceutical applications. Here we report a microwave-directed synthesis of a variety of modified uracil and cytosine nucleobases with high yields under solvent-free conditions. The reaction yields were further improved by addition of Lewis acid. The crystal structures of 5-isopropyl-6-methyluracil and 6-phenyluracil were also determined.
Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors
El-Tayeb, Ali,Qi, Aidong,Müller, Christa E.
, p. 7076 - 7087 (2007/10/03)
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
Synthesis of an AZT-HEPT hybrid and homologous AzddU derivatives
Larsen, Erik,Danel, Krzysztof,Vaaben, Gitte B.,El-Emam, Ali A.,Pedersen, Erik B.,Nielsen, Claus
, p. 417 - 421 (2007/10/03)
3′-Azido-2′,3′-dideoxyuridines 6 and their corresponding α anomers 5 were syrthesizes by condensation of silylated 6-alkyl and 5,6-dialkyl substituted uracils 2 with methyl 3-azido-5-O-tert-butyldiphenylsilyl-2,3-dideoxy-α,β-D-erythro- pentofuranoside (4). Compounds 5 and 6 were treated with tetrabutylammonium fluoride to obtain the deprotected nucleosides 7 and 8, respectively. Acta Chemica Scandinavica 1996.
