- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00338
(2017/09/27)
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- Synthesis of new trisubstituted 4-aminopiperidines as PAF-receptor antagonists
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Two novel classes of 4-aminopiperidines substituted in the 3-position by groups bearing either a carbamate or a ureido function have been synthesized from ethyl 4-oxo-3-piperidinecarboxylate and 3,3′-iminobis(propanenitrile) , respectively. The key step in this synthesis, the reduction of the piperidinic β-enamino ester or nitrile, occurred readily. In contrast to published works, the free primary amines could be isolated from the corresponding β-amino ester or nitrile. Regioselective amidification of the amino group offered two pairs of diastereoisomers which were successfully separated and identified. Measurement of PAF-receptor antagonist activity gave interesting results with an IC50 close to the micromolar. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Benmehdi, Houcine,Lamouri, Aazdine,Serradji, Nawal,Pallois, Frederique,Heymans, Francoise
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p. 299 - 307
(2008/09/18)
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- Anxiolytic properties of certain annelated [1,2,3]triazolo[1,5-c]pyrimidin-5(6H)-ones
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Modification of the benzodiazepine (BZ) receptor binding template 2-aryl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one by replacement of the annelated benzene ring with various alicyclic and heterocyclic moieties led to novel structures with potent BZ receptor binding affinity. High affinity was found in some cycloalkyl-annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones and in some 7,8,9,10-tetrahydropyrido[3,4-e][1,2,4]triazolo[1,5-c] pyrimidin-5(6H)-ones, in which the degree of activity was strongly dependent on the N-substituent in the 9-position. Nine compounds with BZ receptor IC50 binding affinity values equal or superior to diazepam were evaluated in secondary screening. One of these, 9-benzyl-2-phenyl-7,8,9,10-tetrahydropyrido[3,4-e] [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one, showed good activity in rats as a potential anxiolytic agent without sedative liability. However, it increased the rotorod deficit produced by ethanol at anxiolytic doses, an indication of alcohol interaction. Thus, none of the compounds showed an advantage over CGS 9896 (Yokoyama et al. J. Med. Chem. 1982, 25, 337-339), which is free of sedative and alcohol interaction potential as measured by the test procedures described.
- Francis,Bennett,Hyun,Rovinski,Amrick,Loo,Murphy,Neale,Wilson
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p. 2899 - 2906
(2007/10/02)
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