4668
A. Samadi et al. / European Journal of Medicinal Chemistry 46 (2011) 4665e4668
naphthyridine core seems to be a more promising hit. However, no
clear SAR can be deduced from these results, and a careful molec-
ular modeling analysis in progress should possibly afford the keys
in order to rationalize the observed inhibition trends.
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¼
41 ꢀ 7 M)]. We conclude that the most sensitive moiety to
m
modulate AChE inhibition is the length of the spacer, which would
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in our current research programme targeted to the preparation of
new molecules for the potential treatment of AD. Work is now in
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Acknowledgments
[30] J. Marco-Contelles, R. León, C. de los Ríos, A. Samadi, M. Bartolini, V. Andrisano,
O. Huertas, X. Barril, F.J. Luque, M.I. Rodríguez-Franco, B. López, M.G. López,
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formyl-2-(methyl(prop-2-yn-1-yl)amino)-4-phenylnicotinonitrile (32) with
4-(1-benzylpiperidin-4-yl)butan-2-one (31), while compound 10 was obtained as
the only product in a similar reaction between 6-amino-5-formyl-2-(methyl(-
prop-2-yn-1-yl)amino)nicotinonitrile (33) and ketone 31 (Supplementary data).
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A. Samadi thanks CSIC for a I3P-post-doc contract. M. Chioua
thanks ISCIII (MICINN) for a “Sara Borrell” post-doctoral contract. J.
Marco-Contelles thanks MICINN (SAF2006-08764-C02-01, SAF2009-
07271) and CAM (S/SAL-0275-2006) financial support. C. de los Ríos
thanks ISCIII for a “Miguel Servet” contract and financial support
(Fundación CIEN and “Miguel Servet Program”).
Appendix. Supplementary data
Supplementary data associated with this article can be found, in
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