RP 73163: A bioavailable alkylsulphinyl-diphenylimidazole ACAT inhibitor 1

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 1, 1996, Pages 47-50

  Smith, C ^a   Ashton, M J ^a   Bush, R C ^a   Facchini, V ^a   Harris, N V ^a   Hart, T W ^a   Jordan, R ^a   MacKenzie, R ^a   Riddell, D ^a  

^a SANOFI   (France)

Author keywords

[No Author keywords available]

Indexed keywords

2 [5 (3,5 DIMETHYL 1 PYRAZOLYL)PENTYLSULFINYL] 4,5 DIPHENYLIMIDAZOLE; CHOLESTEROL ACYLTRANSFERASE; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; DRUG METABOLITE; ENZYME INHIBITOR; RP 76076; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTERY WALL; ARTICLE; BIOAVAILABILITY; CONTROLLED STUDY; DOG; DRUG BLOOD LEVEL; DRUG METABOLISM; DRUG SYNTHESIS; ENANTIOMER; ENZYME ACTIVITY; ENZYME INHIBITION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYPERCHOLESTEROLEMIA; INTESTINE; LIVER; MACROPHAGE; NONHUMAN; ORAL DRUG ADMINISTRATION; RABBIT; RAT;

EID: 0030021607     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(95)00555-8     Document Type: Article

References (17)

1. Presented in part at the RSC-SCI 7th Medicinal Chemistry Symposium Cambridge 12-15th September, P45, 1993
2. Eur.Pat. 391796 (10 October 1990).
3. Eur.Pat. 372445 (13 June 1990).
4. Ashton, M.J.; Bridge, A.W.; Bush, R.C.; Dron, D.I.; Harris, N.V.; Jones, G.D.; Lythgoe, D.J.; Riddell, D.; Smith, C. Bioorg. Med. Chem. Lett., 1992, 2, 375.
5. Harris, N.V.; Smith, C.; Ashton, M.J.; Bridge, A.W.; Bush, R.C.; Coffee, E.J.; Dron, D.I.; Harper, M.F.; Lythgoe, D.J.; Newton, C.G.; Riddell, D. J. Med. Chem., 1992, 55, 4384.
6. Sliskovic, D.R.; Trivedi, B.K. Current Med. Chem., 1994, 1, 204.
7. Wilde, R.G.; Billheimer, J.T.; Germain, S.J.; Gillies, P.J.; Higley, A.; Kezar III, H.S.; Maduskuie, T.P.; Shimshick, E.S.; Wexler, R.R. Bioorg. Med. Chem. Lett., 1995, 5, 167.
8. Wilde, R.G.; Billheimer, J.T. Bioorg. Med. Chem. Lett., 1995, 5, 173.
9. Wilde, R.G.; Klaczkiewicz, J.D.; Billheimer, J.T.; Wexler, R.R. Bioorg. Med. Chem. Lett., 1995, 5, 177.
10. Separation of the enantiomers of RP 75214 was carried out using a "chiracel OD" column. Typical conditions were: methanol, isopropanol and n-heptane 5:2:93, v/v.
11. Pitchen, P. Chemistry & Industry, 1994, 636. Pitchen. P.; France, C.J.; McFarlane, I.M.; Newton, G.G.; Thompson, D.M. Tet. Letters, 1994, 35, 485.
12. Pitchen, P. Chemistry & Industry, 1994, 636. Pitchen. P.; France, C.J.; McFarlane, I.M.; Newton, G.G.; Thompson, D.M. Tet. Letters, 1994, 35, 485.
13. Chauhan, P.B.; Facchini, V.; Gunraj, P.E.; Hoff, T.A.; Jones, G.D.; Acott, S. Fifth European ISSX Meeting Tours, France. September 26-29, 1993.
14. Warne, P. Society of Pharmaceutical Medicine: Antiatherosclerotic & Lipid Modifying Drugs in the 1990's, London 28-29th October 1993.
15. Dominick, M.A.; Bobrowski, W.A.; MacDonald, J.R.; Roth, B.D.; Wilson, M.W.; Hamelehe, K.L.; Krause, B.R.; Stanfield, R.L. Toxicol. Pathol., 1993, 21, 54.
16. O'Brien, P.M.; Sliskovic, D.R.; Blankley, C.J.; Gough, A.W.. J. Med. Chem., 1994, 37, 1810.
17. Astles, P., submitted to J. Med. Chem.