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Structure Activity Relationships of New Inhibitors of Mammalian 2,3-Oxidosqualene Cyclase Designed from Isoquinoline Derivatives

Autor: Jean Binet, Daniel De Fornel, Patrice Renaut, Didier Thomas, Abdellah Benmbarek

Publikováno v: Chemical and Pharmaceutical Bulletin. 50:316-329

We have designed more potent inhibitors from the previously reported LF 05-0038, a 6-isoquinolinol based inhibitor of 2,3-oxidosqualene cyclase (IC50: 1.1 microM). Replacement of the 3-OH group by various 3-substituted amino groups, and modification

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc4780d151d55b9d062ccb6130641614
https://doi.org/10.1248/cpb.50.316

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Preferential pharmacological inhibition of macrophage ACAT increases plaque formation in mouse and rabbit models of atherogenesis

Autor: Takeo Matsukura, Jean Claude Ortuno, Shigeo Ohbayashi, Alan D Edgar, Jean Binet, Akihiro Matsuura, Thierry Laugel, Paul Padovani, Christiane Legendre, Christian Guffroy, Stéphane Perrey, Francois Bellamy, Toshiya Tanaka

Publikováno v: Atherosclerosis. 155:359-370

The cholesteryl ester, foam cell-enriched vulnerable plaque is a principle pharmacological target for reducing athero-thrombosis. Acyl CoA:cholesterol Acyl Transferase (ACAT) catalyzes the esterification of free cholesterol in intestine, liver, adren

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df4c207d5c2d93cf5f4bbecd4b5d2dd9
https://doi.org/10.1016/s0021-9150(00)00599-2

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Structural and Stereoelectronic Requirements for the Inhibition of Mammalian 2,3-Oxidosqualene Cyclase by Substituted Isoquinoline Derivatives

Autor: Martine Barth, Patrice Renaut, S. Samreth, Francis Schuber, Jean Binet, Daniel De Fornel, Didier Thomas

Publikováno v: Journal of Medicinal Chemistry. 39:2302-2312

2,3-Oxidosqualene lanosterol-cyclase (OSC; EC 5.4.99.7) is an attractive target for the design of compounds that block hepatic cholesterol biosynthesis. (4a alpha, 5 alpha, 6 beta, 8a beta)-Decahydro-5,8a-dimethyl-2-(1,5,9-trimethyldecyl)-6- isoquino

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbe886c509b1f15ac31d1d33edd8642f
https://doi.org/10.1021/jm9504621

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ChemInform Abstract: Structure-Activity Relationships of New Inhibitors of Mammalian 2,3-Oxidosqualene Cyclase Designed from Isoquinoline Derivatives

Autor: Daniel De Fornel, Patrice Renaut, Abdellah Benmbarek, Jean Binet, Didier Thomas

Publikováno v: ChemInform. 33

We have designed more potent inhibitors from the previously reported LF 05-0038, a 6-isoquinolinol based inhibitor of 2,3-oxidosqualene cyclase (IC50: 1.1 μM). Replacement of the 3-OH group by various 3-substituted amino groups, and modification of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::881fa798471a8005dc1e947df66fa7b9
https://doi.org/10.1002/chin.200232137

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Synthesis of a series of compounds related to betaxolol, a new .beta.1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases

Autor: Philippe Manoury, Jean Binet, Jean Rousseau, Françoise Lefèvre-Borg, I Cavero

Publikováno v: Journal of Medicinal Chemistry. 30:1003-1011

A series of para-substituted phenoxypropanolamines has been synthesized and tested for beta-adrenoceptor blocking activity. Some derivatives (8, 11, 12, 20, 21) exhibited greater in vitro potency than the reference drugs metoprolol and propranolol. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6448962b3e6a9e4841132796c73008af
https://doi.org/10.1021/jm00389a008

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Synthesis and antihypertensive activity of a series of 4-amino-6,7-dimethoxyquinazoline derivatives

Autor: Andre Pierre Fernand Dumas, I Cavero, Philippe Manoury, Françoise Lefèvre-Borg, Jean Binet

Publikováno v: Journal of medicinal chemistry. 29(1)

A series of N2-[(acylamino)alkyl]-6,7-dimethoxy-2,4-quinazolinediamines was synthesized as potential alpha 1-adrenoceptor antagonists. When administered to spontaneously hypertensive rats at 10 mg/kg po, a number of propanediamine derivatives showed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f7dff340d92fc360619058bcec3adce
https://pubmed.ncbi.nlm.nih.gov/3941410

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ChemInform Abstract: Synthesis and Antihypertensive Activity of a Series of 4-Amino-6,7-dimethoxyquinazoline Derivatives

Autor: I Cavero, Françoise Lefèvre-Borg, Andre Pierre Fernand Dumas, Jean Binet, Philippe Manoury

Publikováno v: Chemischer Informationsdienst. 17

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::53bf6c08bfbeb29f4097f9cce9eb1967
https://doi.org/10.1002/chin.198620220

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