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Titolo:
Novel hydroxyphenylurea dual inhibitor against acyl-CoA: Cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent
Autore:
Nakao, K; Kubota, H; Yasuhara, M; Saito, K; Suzuki, T; Ohmizu, H; Shimizu, R;
Indirizzi:
Tanabe Seiyaku Co Ltd, Discovery Res Lab, Osaka 5328505, Japan Tanabe Seiyaku Co Ltd Osaka Japan 5328505 Res Lab, Osaka 5328505, Japan Tanabe Seiyaku Co Ltd, Discovery Res Lab, Toda, Saitama 3358505, Japan Tanabe Seiyaku Co Ltd Toda Saitama Japan 3358505 , Saitama 3358505, Japan
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 4, volume: 9, anno: 2001,
pagine: 853 - 861
SICI:
0968-0896(200104)9:4<853:NHDIAA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
ATHEROSCLEROSIS; ANTIOXIDANTS; PATHOGENESIS; DERIVATIVES; MACROPHAGES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Shimizu, R Tanabe Seiyaku Co Ltd, Discovery Res Lab, 2-2-50 Kawagishi, Osaka 5328505,Japan Tanabe Seiyaku Co Ltd 2-2-50 Kawagishi Osaka Japan 5328505 pan
Citazione:
K. Nakao et al., "Novel hydroxyphenylurea dual inhibitor against acyl-CoA: Cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent", BIO MED CH, 9(4), 2001, pp. 853-861

Abstract

Novel hydroxyphenylurea derivatives were synthesized and their inhibitory potency evaluated against acyl-CoA: cholesterol acyltransferase (ACAT). Quantitative structure-activity relationship analysis revealed that their ACATinhibitory activities were controlled by the hydrophobicity of the whole molecule, the substitution pattern of urea moiety. and the existence of carboxylic acid. The derivatives with strong activities inhibited foam cell formations. Moreover. these compounds showed antioxidative effects against lowdensity lipoprotein (LDL). owing to their characteristic 3-tert-butyl-2-hydroxy-5-methoxyphenyl substructure. Based on the mechanism of atherosclerosis generation, this hydroxyphenylurea-type dual inhibitor against both ACATand LDL oxidation is expected to be a promising drug for atherosclerosis. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/01/20 alle ore 07:32:49