- Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors
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Adenosine kinase (AK) is the primary enzyme responsible for adenosine metabolism. Inhibition of AK effectively increases extracellular adenosine concentrations and represents an alternative approach to enhance the beneficial actions of adenosine as compared to direct-acting receptor agonists. Clitocine (3), isolated from the mushroom Clitocybe inversa, has been found to be a weak inhibitor of AK. We have prepared a number of analogues of clitocine in order to improve its potency and demonstrated that 5′-deoxy-5′-amino-clitocine (7) improved AK inhibitory potency by 50-fold.
- Lee, Chih-Hung,Daanen, Jerome F,Jiang, Meiqun,Yu, Haixia,Kohlhaas, Kathy L,Alexander, Karen,Jarvis, Michael F,Kowaluk, Elizabeth L,Bhagwat, Shripad S
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p. 2419 - 2422
(2007/10/03)
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- NOVEL PYRIMIDINE DERIVATIVES EFFICACIOUS AS PSYCHOTROPIC DRUG AND PROCESS FOR THE PRODUCTION THEREOF
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A compound represented by the formula, or a pharmacologically acceptable salt thereof: wherein A1is a halogen atom, a lower alkyl group, a cycloalkyl group, a substituted lower alkyl group or a substituted cycloalkyl group; B1and Bs
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- A convenient synthesis of 4,6-dichloro-5-benzylthiopyrimidine
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A practical and convenient two-step synthesis of the title compound 4,6-dichloro-5-benzylthiopyrimidine from 4,6-dihydroxypyrimidine is described.
- Thang,Watson,Best,Fam,Keep
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p. 2363 - 2369
(2007/10/02)
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- Ylides of Heterocycles. VII. . I-, N-, P- and S-Ylides of Pyrimidones
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The reaction of pyrimidone derivatives 1a-d with iodosobenzene prepared in situ from diacetoxyiodobenzene or dichloroiodobenzene afforded the iodonium-ylides 2a-d in good yields.Their thermal rearrangement produced 5-iodo-4-phenoxy-pyrimidin-6(1H)-ones 3a-c.Reductive deiodination of 3 gave the corresponding 4-phenoxypyrimidin-6(1H)-ones 4a-c.Acid catalized treatment of the iodonium-ylides 2a-d with nucleophiles such as pyridine, nicotinamide, isoquinoline, or triphenylphosphine produced the corresponding N- or P-ylides 7, 8, 9, and 10, respectively.The thiophanium-ylides 11a,c were obtained from the iodonium-ylides 2 without the use of a catalyst.The pyridinium-ylides 7 have also been prepared from the 5-halopyrimidones 5 or 6 which in turn could be obtained from the reactive iodonium-ylides 2 with hydrochloric or hydrobromic acid, respectively.
- Habib, Nargues Samuel,Kappe, Thomas
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p. 385 - 388
(2007/10/02)
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