- PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP - PLA2
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The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema (I).
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Page/Page column 27
(2012/06/30)
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- Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
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NAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD+ biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD+ level. In this report, a series of structural analogs of FK866 (1), a known NAmPRTase inhibitor, was synthesized and tested for inhibitory activities against the proliferation of cancer cells and human NAmPRTase. Among them, compound 7 showed similar anti-cancer and enzyme inhibitory activities to compound 1. Further investigation of compound 7 with X-ray analysis revealed a co-crystal structure in complex with human NAmPRTase, suggesting that Asp219 in the active site of the enzyme could contribute to an additional interaction with the pyrrole nitrogen of compound 7.
- You, Hyun,Youn, Hyung-Seop,Im, Isak,Bae, Man-Ho,Lee, Sang-Kook,Ko, Hyojin,Eom, Soo Hyun,Kim, Yong-Chul
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experimental part
p. 1153 - 1164
(2011/04/17)
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- A preparative route to methyl 3-(heteroaryl)acrylates using Heck methodology
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Methyl 3-(heteroaryl)acrylates were prepared using Heck coupling of heteroarene halides with methyl acrylate mediated by Pd(OAc)2/ P(OCH3)3. Reactions were highly efficient (reaction times between 60 and 120 min) and scalable to 100 g of heteroarene halide. The isolated yields are from 76 to 99%.
- Kwok, Thomas J.,Virgilio, Joseph A.
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p. 694 - 696
(2012/12/25)
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