INHIBITORS OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT) AS HYPOCHOLESTEROLEMIC AGENTS .14. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A NOVEL SERIES OF SULFONAMIDE TETRAZOLES

被引：3

作者：

LEE, HT ^{[1
]}

SLISKOVIC, DR ^{[1
]}

STANFIELD, RL ^{[1
]}

HAMELEHLE, KL ^{[1
]}

BOUSLEY, RF ^{[1
]}

KRAUSE, BR ^{[1
]}

机构：

[1] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT ATHEROSCLEROSIS THERAPEUT,ANN ARBOR,MI 48105

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 03期

关键词：

D O I：

10.1016/0960-894X(95)00026-P

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 and/or the secretion of VLDL by the Liver and therefore provide a therapy for the treatment of hypercholesterolemia and atherosclerosis in man.

引用

页码：301 / 306

页数：6

共 21 条

[1] INHIBITORS OF ACYL-COA CHOLESTEROL ACYLTRANSFERASE .5. IDENTIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL BETA-KETOAMIDES AS HYPOCHOLESTEROLEMIC AGENTS [J].

AUGELLISZAFRAN, CE ;

BLANKLEY, CJ ;

ROTH, BD ;

TRIVEDI, BK ;

BOUSLEY, RF ;

ESSENBURG, AD ;

HAMELEHLE, KL ;

KRAUSE, BR ;

STANFIELD, RL .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (20) :2943-2949

[2] SYNTHESIS OF 3-SULFOPROPIONIMIDE [J].

BECK, ML .

JOURNAL OF ORGANIC CHEMISTRY, 1968, 33 (02) :897-&

[3]

BERNSTEIN PR, 1987, SYNTHESIS-STUTTGART, P1133

[4] COMPARISON OF CI-976, AN ACAT INHIBITOR, AND SELECTED LIPID-LOWERING AGENTS FOR ANTIATHEROSCLEROTIC ACTIVITY IN ILIAC FEMORAL AND THORACIC AORTIC LESIONS - A BIOCHEMICAL, MORPHOLOGICAL, AND MORPHOMETRIC EVALUATION [J].

BOCAN, TMA ;

MUELLER, SB ;

UHLENDORF, PD ;

NEWTON, RS ;

KRAUSE, BR .

ARTERIOSCLEROSIS AND THROMBOSIS, 1991, 11 (06) :1830-1843

[5] LIPOPROTEIN METABOLISM IN THE MACROPHAGE - IMPLICATIONS FOR CHOLESTEROL DEPOSITION IN ATHEROSCLEROSIS [J].

BROWN, MS ;

GOLDSTEIN, JL .

ANNUAL REVIEW OF BIOCHEMISTRY, 1983, 52 :223-261

[6]

COBBE SM, 1993, BRIT HEART J, V69, pS63

[7]

DAVIES SW, 1993, BRIT HEART J, V69, P3

[8]

GRUNDY SM, 1972, GASTROENTEROLOGY, V62, P1200

[9] EFFECTS OF THE ACAT INHIBITOR CL-277,082 ON CHOLESTEROL-METABOLISM IN HUMANS [J].

HARRIS, WS ;

DUJOVNE, CA ;

VONBERGMANN, K ;

NEAL, J ;

AKESTER, J ;

WINDSOR, SL ;

GREENE, D ;

LOOK, Z .

CLINICAL PHARMACOLOGY & THERAPEUTICS, 1990, 48 (02) :189-194

[10] THE 1,2,4-THIADIZINE RING SYSTEM .1. THE SYNTHESIS OF 1,2,4,2H-THIADIAZINE-3,5(4H,6H)-DIONE-1,1-DIOXIDE [J].

HINMAN, RL ;

LOCATELL, L .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1959, 81 (21) :5655-5658

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