4612
F. Vergne et al. / Bioorg. Med. Chem. Lett. 14 (2004) 4607–4613
Scheme 2. Reagents and conditions: (a) RCONH2, (R@Me or H), 1-methyl-2-pyrrolidinone, 200°C; (b) methyl-1-methylhydrazine carbodithioate,
DMF, TOTU, 0°C; (c) TMSOTf, toluene, <40°C; (d) cyclohexylamine, EtOH, reflux; (e) SOCl2, toluene; (f) NH3, 1,4-dioxane, D.
Physiol. Lung Cell. Mol. Physiol. 2003, 284, L279–
L289.
inhibitory activity and exhibiting high selectivity over
PDE4. The findings from this study will be useful for
further optimization of these newly discovered chemical
leads, which will be the subject of additional reports in
due course.
5. (a) Perez-Torres, S.; Cortes, R.; Tolnay, M.; Probst, A.;
Palacios, J. M.; Mengod, G. Exp. Neurol. 2003, 182,
322–334; (b) Miro, X.; Perez-Torres, S.; Palacios, J. M.;
Puigdomenech, P.; Mengod, G. Synapse 2001, 40,
201–214; (c) Sasaki, T.; Kotera, J.; Omori, K. Biochem.
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Acknowledgements
6. Lee, R.; Wolda, S.; Moon, E.; Esselstyn, J.; Hertel, C.;
Lerner, A. Cell. Signal. 2002, 14, 277–284.
We thank the scientists from the Analytical Support
Group for their help in compound characterization and
Professor Anthony G. M. Barrett for helpful discussions
regarding the thiadiazole chemistry. We also thank the
Evotec OAI scientists for their assistance in this project.
7. (a) Kotera, J. PDE7- news and views, William Harvey
Research Conferences, Porto, Portugal, Dec 5–7, 2001; (b)
Kluxen, F. W. PCT int. Appl. WO 0183772 A1, 2001.
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