Výsledky vyhledávání - "Acyl CoA cholesterol O acyltransferase"

Brain Targeting of Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor K-604 via the Intranasal Route Using a Hydroxycarboxylic Acid Solution

Autor: Noriko Noguchi, Yasuomi Urano, Masayoshi Miyamoto, Yoshihiko Tsunenari, Shin-ichiro Ogawa, Kimiyuki Shibuya, Shigeru Morikawa

Publikováno v: ACS Omega
ACS Omega, Vol 4, Iss 16, Pp 16943-16955 (2019)

An acyl-CoA:cholesterol O-acyltransferase-1 (ACAT-1/SOAT-1) inhibitor, K-604 is a promising drug candidate for the treatment of Alzheimer's disease and glioblastoma; however, it exhibits poor solubility in neutral water and low permeability across th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fad4fe7cc5ca6aef1b49bda38aade33
http://europepmc.org/articles/PMC6796924

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Statin Therapy Alone and in Combination with an Acyl-CoA:Cholesterol O-Acyltransferase Inhibitor on Experimental Atherosclerosis

Autor: John T. Fallon, Valentin Fuster, Juan J. Badimon, Zahi A. Fayad, Stephen G. Worthley, Gérard Helft, Matthew I. Worthley, Roberto Corti, Derek P. Chew, Azfar Zaman

Publikováno v: Pathophysiology of Haemostasis and Thrombosis. 36:9-17

The ability to modify the enzymatic processes involved in promoting atherosclerotic plaque disruption and to serially monitor atherosclerotic evolution could provide novel information in the management of patients with atherosclerosis. We studied the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::47305c79301dab098d4208f687e30729
https://doi.org/10.1159/000112634

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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

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Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)

Autor: Rika Obata, Yoshihiro Harigaya, Satoshi Ōmura, Hiroshi Tomoda, Toshiaki Sunazuka

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2683-2688

Modification and structure-activity relationships of ACAT inhibitor pyripyropene were examined. PR-109 (7g) showed the most potent (IC50 = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activity (IC50 = 19 nM) and its in vivo activi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::558c3f13c0d3850b718a95c90653e866
https://doi.org/10.1016/0960-894x(95)00451-x

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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

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ChemInform Abstract: Tetrazole-Substituted Ureas as Inhibitors of Acyl-CoA:Cholesterol O- Acyltransferase (ACAT). A Novel Preparation of Ureas from Weakly Nucleophilic Amines

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

Publikováno v: ChemInform. 27

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5d4222255aef58ba3d365f4e7ce47b99
https://doi.org/10.1002/chin.199649149

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ChemInform Abstract: Synthesis, X-Ray Crystal Structure, and Biological Activity of FR186054, a Novel, Potent, Orally Active Inhibitor of Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) Bearing a Pyrazole Ring

Autor: Noriko Ishibe, Hiroyuki Hagihara, Masae Sawada, Akira Tanaka, Hirokazu Tanaka, Takeshi Terasawa, Yuri Sakuma, Takayoshi Kinoshita, Hisashi Takasugi

Publikováno v: ChemInform. 29

The synthesis, single crystal X-ray structural analysis, and biological activity of FR186054 (2c), a new, potent, orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT), containing a pyrazole ring are described. This compound d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::98fa67dd4e0d8f3b0c6d425f6d4e1069
https://doi.org/10.1002/chin.199818150

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