Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): Synthesis and initial structure-activity relationships

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 7, 2005, Pages 1829-1833

  Kempson, James ^a   Pitts, William J ^a   Barbosa, Joseph ^a   Guo, Junqing ^a   Omotoso, Omonike ^a   Watson, Andrew ^a   Stebbins, Karen ^a   Starling, Gary C ^a   Dodd, John H ^a   Barrish, Joel C ^a   Felix, Raymond ^b   Fischer, Karl ^b  

^a BRISTOL MYERS SQUIBB   (United States)

^b Cambridge Discovery Chemistry   (United States)

Author keywords

PDE7; Pyrimidine

Indexed keywords

PHOSPHODIESTERASE; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE VII; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG SOLUBILITY; DRUG SYNTHESIS; IC 50; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; STRUCTURE ACTIVITY RELATION;

EID: 20144366973     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.02.025     Document Type: Article

References (12)

1. S.H. Francis, I.V. Turko, and J.D. Corbin Prog. Nucleic Acid Res. Mol. Biol. 65 2001 1
2. L. Li, C. Yee, and J.A. Beavo Science 283 1999 848
3. R. Lee, S. Wolda, E. Moon, J. Esselstyn, C. Hertel, and A. Lerner Cell. Signalling 14 2002 277
4. S.J. Smith, S. Brookes-Fazakerley, L.E. Donnelly, P.J. Barnes, M.S. Barnette, and M.A. Giembycz Am. J. Physiol. Lung Cell Mol. Physiol. 284 2002 L279
5. G. Yang, K.W. McIntyre, R.M. Townsend, H.H. Shen, W.J. Pitts, J.H. Dodd, S.G. Nadler, M. McKinnon, and A.J. Watson J. Immunol. 171 2003 6414
6. A. Martinez, A. Castro, C. Gil, M. Miralpeix, V. Segarra, T. Domenech, J. Beleta, J.M. Palacious, H. Ryder, X. Miro, C. Bonet, J.M. Casacuberta, F. Azorin, B. Pina, and P. Puigdomenech J. Med. Chem. 46 2000 683
7. M.J. Barnes, N. Cooper, R.J. Davenport, H.J. Dyke, F.P. Galleway, F.C.A. Galvin, L. Gowers, A.F. Haughan, C. Lowe, J.W.G. Meissner, J.G. Montana, T. Morgan, C.L. Picken, and R.J. Watson Bioorg. Med. Chem. Lett. 11 2001 1081
8. F. Vergne, P. Bernardelli, E. Lorthiois, N. Pham, E. Proust, C. Oliveira, A.-K. Mafroud, F. Royer, R. Wrigglesworth, J. Schellhaas, M. Barvian, F. Moreau, M. Idrissi, A. Tertre, B. Bertin, M. Coupe, P. Berna, and P. Soulard Bioorg. Med. Chem. Lett. 14 2004 4607
9. E. Lorthiois, P. Bernardelli, F. Vergne, C. Oliveira, A.-K. Mafroud, E. Proust, L. Heuze, F. Moreau, and P. Idrissi Bioorg. Med. Chem. Lett. 14 2004 4623
10. W.J. Pitts, W. Vaccaro, T. Huynh, K. Leftheris, J.Y. Roberge, J. Barbosa, J. Guo, B. Brown, A. Watson, K. Donaldson, G.C. Starling, P.A. Kiener, M.A. Poss, J.H. Dodd, and J.C. Barrish Bioorg. Med. Chem. Lett. 14 2004 2955
11. M. Kansy, F. Senner, and K. Gubernator J. Med. Chem. 41 1998 1007
12. Attempts to obtain CACO-2 data on compounds 2a-k were unsuccessful due to low solubility in the assay buffer