Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 11, 2006, Pages 3039-3042

  Li, Jin ^a   Bertinato, Peter ^a   Cheng, Hengmiao ^a   Cole, Bridget M ^a   Bronk, Brian S ^a   Jaynes, Burton H ^a   Hickman, Anne ^a   Haven, Michelle L ^a   Kolosko, Nicole L ^a   Barry, Chris J ^a   Manion, Tara B ^a  

^a PFIZER INC   (United States)

Author keywords

Microsomal triglyceride transfer protein; MTP; Obesity

Indexed keywords

ANTIOBESITY AGENT; MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN INHIBITOR;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DETERMINATION; DRUG EFFICACY; DRUG INDICATION; DRUG MECHANISM; DRUG POTENCY; DRUG RETENTION; DRUG SCREENING; DRUG SYNTHESIS; IN VIVO STUDY; INTESTINE; MOUSE; NONHUMAN; OBESITY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-OBESITY AGENTS; CARRIER PROTEINS; MICE; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA; MURINAE;

EID: 33646071789     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.02.058     Document Type: Article

References (25)

1. Pfizer Animal Health Data File.
2. Armstrong P.J., and Lund E.M. Vet. Clin. Nutr. 3 (1996) 83
3. Burkholder W.J., and Bauer J.E. J. Am. Vet. Chem. Assoc. 212 (1998) 658
4. Edney A.T., and Smith P.M. Vet. Rec. 118 (1986) 391
5. Kassab S., Patterson S., Wilkins F.C., Mizelle H.L., Reinhart G.A., and Granger J.P. Hypertension 23 (1994) 997
6. Mason E. Vet. Rec. 86 (1970) 612
7. Mattheeuws D., Rottiers R., Kaneko J.J., and Vermeulen A. Am. J. Vet. Res. 45 (1984) 98
8. Mattheeuws D., Rottiers R., and Baeyens D. J. Am. Anim. Hosp. Assoc. 20 (1990) 287
9. Panciera D.L., Thomas C.B., Eicker S.W., and Atkins C.E. J. Am. Vet. Med. Assoc. 197 (1990) 1504
10. Robertson I.D. Prev. Vet. Med. 40 (1999) 75
11. Scarlett J.M., and Donoghue S. J. Am. Vet. Med. Assoc. 212 (1998) 1725
12. Wetterau J.R., Lin M.C., and Jamil H. Biochim. Biophys. Acta 1345 (1997) 136
13. Gordon D.A., Wetterau J.R., and Gregg R.E. Trends Cell Biol. 5 (1995) 317
14. Olofsson S.O., Asp L., and Boren J. Curr. Opin. Lipidol. 10 (1999) 341
15. Wetterau J.R., Gregg R.E., Harrity T.W., Arbeeny C., Cap M., Connolly F., Chu C.-H., George R.J., Gordon D.A., Jamil H., Jolibois K.G., Kunselman L.K., Lan S.-J., Maccagnan T.J., Ricci B., Yan M., Young D., Chen Y., Fryszman O.M., Logan J.V.H., Musial C.L., Poss M.A., Robl J.A., Simpkins L.M., Slusarchyk W.A., Sulsky R., Taunk P., Magnin D.R., Tino J.A., Lawrence R.M., Dickson J.K., and Biller S.A. Science 282 (1998) 751
16. Chandler, C. E.; Hickman, M. A.; Lundy, K. M.; Morgan, B. P. EP1099439A2, 2001.
17. Chandler C.E., Wilder D.E., Pettini J.L., Savoy Y.E., Petras S.F., Chang G., Vincent J., and Harwood H.J. J. Lipid Res. 44 (2003) 1887
18. Iglesias P., and Diez J.J. Expert Opin. Investig. Drugs 12 (2003) 1777
19. Sorbera L.A., Martin L., Silvestre J., and Castaner J. Drugs Future 25 (2000) 1138
20. Roevens P., Heeres J., Meerpoel L., Dupont A., and Borghys H. Atherosclerosis 144 Suppl. 1 (1999) 38
21. Ksander G.M., deJesus R., Yuan A., Fink C., Moskal M., Carlson E., Kukkola P., Bilci N., Wallace E., Neubert A., Feldman D., Mogelesky T., Poirier K., Jeune M., Steele R., Wasvery J., Stephan Z., Cahill E., Webb R., Navarrete A., Lee W., Gilbson J., Alexander N., Sharif H., and Hospattankar A. J. Med. Chem. 44 (2001) 4677
22. Robl J.A., Sulsky R., Sun C.-Q., Simpkins L.M., Wang T., Dickson J.K., Chen Y., Magnin D.R., Taunk P., Slusarchyk W.A., Biller S.A., Lan S.-J., Connolly F., Kunselman L.K., Sabrah T., Jamil H., Gordon D., Harrity T.W., and Wetterau J.R. J. Med. Chem. 44 (2001) 851
23. Bertinato, P.; Blize, A. E.; Bronk, B. S.; Cheng, H.; Huatan, H.; Li, J.; Mason, C. P. WO 2003002533, 2003.
24. Bertinato, P.; Bronk, B. S.; Cheng, H.-M.; Chang, G.; Cole, B. M.; Li, J.; Ruggeri, R. B. WO 2004056777, 2004.
25. 50 values are obtained using standard methods and first order kinetic calculations.