Non thiazolidinedione antihyperglycaemic agents. 2: α-carbon substituted β-phenylpropanoic acids

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 17, 1996, Pages 2127-2130

  Buckle, D R ^a   Cantello, B C C ^a   Cawthorne, M A ^a   Coyle, P J ^a   Dean, D K ^a   Faller, A ^a   Haigh, D ^a   Hindley, R M ^a   Jefcott, L J ^a   Lister, C A ^a   Pinto, I L ^a   Rami, H K ^a   Smith, D G ^a   Smith, S A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 0001294801     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00382-4     Document Type: Article

References (11)

1. For part 1 see Buckle, D. R.; Cantello, B. C. C.; Cawthorne, M. A.; Coyle, P. J.; Dean, D. K.; Faller, A.; Haigh, D.; Hindley, R. M.; Jefcott, L. J.; Lister, C. A.; Pinto, I. L.; Rami, H. K.; Smith, D. G. and Smith, S. A., Bioorg. Med. Chem. Lett., Preceding paper.
2. Cantello, B. C. C.; Cawthorne, M. A.; Cottam, G. P.; Duff, P. T.; Haigh, D.; Hindley, R. M.; Lister, C. A.; Smith, S. A. and Thurlby, P. L., J. Med. Chem., 1994, 37, 3977-3985.
3. Haigh, D. and Rami, H. K., International Patent Appl., Publication No. WO94/13650, 1994.
4. -1 diet) which reduces the area under the glucose tolerance curve by 25% relative to controls.
5. Rami, H. K., International Patent Appl., Publication No. WO95/03288, 1995.
6. Yoshioka, T.; Fujita, T.; Kanai, T.; Aizawa, Y.; Kurumada, T.; Hasegawa, K. and Horikoshi, H., J. Med. Chem., 1989, 32, 421-428.
7. (a) Lehmann, J. M.; Moore, L. B.; Smith-Oliver, T. A.; Wilkison, W. O.; Willson, T. M. and Kliewer, S. A., J. Biol. Chem., 1995, 270, 12953-12956.
8. (b) Forman, B. M.; Tontonoz, P.; Chen, J.; Brun, R. P.; Spiegelman, B. M. and Evans, R. M., Cell, 1995, 83, 803-812.
9. (c) Willson, T. M.; Cobb, J. E.; Cowan, D. J.; Wiethe, R. W.; Correa, I. D.; Prakash, S. R.; Beck, K. D.; Moore, L. B.; Kliewer, S. A. and Lehmann, J. M., J. Med. Chem., 1996, 39, 665-668.
10. -1 diet in ob/ob mice} was present at 145 pM. Competing compounds were dissolved in DMSO (concentration of DMSO did not exceed 0.1%). Binding was allowed to reach equilibrium by incubation for 18 hours at 4°C. Bound ligand was separated from free on mixed cellulose ester filters. Each assay was performed in triplicate.
11. West, C. T.; Donnelly, S. J.; Kooistra, D. A. and Doyle, M. P., J. Org. Chem., 1973, 38, 2675-2681.