Výsledky vyhledávání - "K. L. Hamelehle"

Influence of membrane partitioning on inhibitors of membrane-bound enzymes

Publikováno v: Journal of Pharmaceutical Sciences. 90:1859-1867

Membrane–water partitioning of inhibitors of acyl-coenzyme A:cholesterol acyltransferase (ACAT) governs the concentration of inhibitor that ACAT is exposed to and determines the corresponding extent of cholesterol esterification inhibition. Partiti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61244ab5adf2ab5b82bfc673fd6d78a4
https://doi.org/10.1002/jps.1135

Zobrazit plný text záznamu

Phospholipase A2 relieves phosphatidylcholine inhibition of micellar cholesterol absorption and transport by human intestinal cell line Caco-2

Autor: Reynold Homan, K. L. Hamelehle

Publikováno v: Journal of Lipid Research. 39:1197-1209

Cholesterol absorption from bile acid micelles is suppressed by phosphatidylcholine (PC) in the micelles. The effects of micellar phospholipid composition on absorption, metabolism, and secretion of lipids were examined in Caco-2 cells incubated with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b71d682d6ce944d413eea240da663bc8
https://doi.org/10.1016/s0022-2275(20)32544-x

Zobrazit plný text záznamu

Inhibitors of Acyl-CoA:Cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: Synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates

Autor: Helen T. Lee, Brian R. Krause, Bruce D. Roth, R. L. Stanfield, W. H. Roark, Joseph Armand Picard, Drago Robert Sliskovic, R. F. Bousley, K. L. Hamelehle

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:289-294

Sulfoacetic acid, phosphoramidate, and phosphoramide analogs of the ACAT inhibitors, CI-999 and CI-1011 were synthesized. The structure-activity relationships of these compounds as ACAT inhibitors are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c74ac58e97453c222e55e48824453b5e
https://doi.org/10.1016/s0960-894x(98)00011-0

Zobrazit plný text záznamu

Inhibitors of acyl-CoA:cholesterol acyltransferase: novel trisubstituted ureas as hypocholesterolemic agents

Autor: R. L. Stanfield, K. L. Hamelehle, Brian R. Krause, Bharat K. Trivedi, A. D. Essenburg, Ann Holmes, Terri S. Purchase, MaryKay Shaw Hes

Publikováno v: Bioorganic & Medicinal Chemistry. 5:739-747

Our continued interest in developing novel, potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors, and our discovery of several active series of disubstituted urea ACAT inhibitors, have led us to investigate a series of trisubstituted ureas t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::548891bbc8028db6dfedefd49fead020
https://doi.org/10.1016/s0968-0896(97)00019-9

Zobrazit plný text záznamu

Tetrazole-substituted ureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). A novel preparation of ureas from weakly nucleophilic amines

Autor: Maureen K. Anderson, Andrew D. White, Thomas M.A. Bocan, R. F. Bousley, Claude Forsey Purchase, Sandra Bak Mueller, Brian R. Krause, Peter Lee, J. F. Reindel, Reynold Homan, R. L. Stanfield, K. L. Hamelehle, Cecilia Speyer

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:1753-1758

A novel series of tetrazole-substituted ureas 2 were prepared from weakly nucleophilic amines using a new coupling method. The ureas were found to potently inhibit liver ACAT in vitro and lower total serum cholesterol in vivo. A comparison of urea 2b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::19c77c667fa12975e42e0099ca9943ab
https://doi.org/10.1016/0960-894x(96)00310-1

Zobrazit plný text záznamu

Inhibitors of acyl-coa:cholesterol acyltransferase (ACAT). 15. sulfonylurea inhibitors with excellent hypocholesterolemic activity in vivo

Autor: Maureen K. Anderson, Reynold Homan, Joseph Armand Picard, R. L. Stanfield, Bruce D. Roth, Brian R. Krause, K. L. Hamelehle, W. Howard Roark, R. F. Bousley

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2367-2370

A series of sulfonylureas were prepared and tested for the ability to inhibit the enzyme acyl-CoA: cholesterol acyltransferase (ACAT) in vitro and lower plasma cholesterol in cholesterol-fed rats in vivo. Although compounds from this series were gene

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f2274c3c7bed1368f9757651e46d528b
https://doi.org/10.1016/0960-894x(95)00408-l

Zobrazit plný text záznamu

A series of conformationally and sterically constrained analogs of N-phenyl-N′-aralkylurea ACAT inhibitors

Autor: R. L. Stanfield, Bharat K. Trivedi, Brian R. Krause, A. D. Essenburg, K. L. Hamelehle, Terri S. Purchase, Ann Holmes, MaryKay Shaw Hes

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2229-2234

A series of conformationally and sterically constrained analogs of N-phenyl-N′-aralkylureas has been synthesized and evaluated as potential ACAT inhibitors. Most of these analogs are potent inhibitors of ACAT in vitro and lower plasma cholesterol i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::17d754d97cd0a5669b8d4f1f88a3209d
https://doi.org/10.1016/0960-894x(95)00387-9

Zobrazit plný text záznamu

Inhibitors of Acyl-CoA:Cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents 14. synthesis and structure-activity relationships of a novel series of sulfonamide tetrazoles

Autor: R. F. Bousley, Brian R. Krause, Helen T. Lee, K. L. Hamelehle, Drago Robert Sliskovic, R. L. Stanfield

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:301-306

The syntheses and biological activities of a series of novel sulfonamide tetrazole derivatives are reported. The ability of these compounds to inhibit ACAT is described. Such agents may decrease the absorption of dietary cholesterol in the intestine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0a21f3fac4508de264a239eb013bc462
https://doi.org/10.1016/0960-894x(95)00026-p

Zobrazit plný text záznamu

Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents. 8. Incorporation of Amide or Amine Functionalities into a Series of Disubstituted Ureas and Carbamates. Effects on ACAT Inhibition in vitro and Efficacy in vivo

Autor: C. J. Blankley, B.R. Krause, Patrick Michael O'brien, Michael William Wilson, K. L. Hamelehle, R. L. Stanfield, D. R. Sliskovic, Bruce David Roth

Publikováno v: Journal of Medicinal Chemistry. 37:1810-1822

A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase in vitro and to lower plasma total cholesterol in a variety of cholesterol-fed rat models

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec94948a126f2e8cc31ae8279ce1bf13
https://doi.org/10.1021/jm00038a010

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání