URACIL-BASED ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：5

作者：

DORSCH, D

MEDERSKI, WWKR

OSSWALD, M

BEIER, N

SCHELLING, P

机构：

[1] E. Merck, Preclinical Pharmaceutical Research

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 18期

关键词：

D O I：

10.1016/0960-894X(95)00370-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1,2,3,4-Tetrahydro-2,4-pyrimidinedione (uracil) is a valuable nucleus for the construction of potent antagonists of the AT(1) angiotensin II receptor. Various synthetic routes were applied in order to introduce a wide range of different groups at the N-3-nitrogen and to obtain condensed uracil derivatives as well. 121 with a N,N-dimethylacetamide residue at N-3 was the most potent compound with an IC50 of 0.65 nM.

引用

收藏

页码：2071 / 2076

页数：6

相关论文

共 22 条

[1] QUINAZOLINONES-1 - DESIGN AND SYNTHESIS OF POTENT QUINAZOLINONE-CONTAINING AT(1)-SELECTIVE ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

ALLEN, EE ;

DELASZLO, SE ;

HUANG, SX ;

QUAGLIATO, CS ;

GREENLEE, WJ ;

CHANG, RSL ;

CHEN, TB ;

FAUST, KA ;

LOTTI, VJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (06) :1293-1298

[2] STUDIES IN CHEMOTHERAPY .10. ANTITHYROID COMPOUNDS - SYNTHESIS OF 5-SUBSTITUTED AND 6-SUBSTITUTED 2-THIOURACILS FROM BETA-OXOESTERS AND THIOUREA [J].

ANDERSON, GW ;

HALVERSTADT, IF ;

MILLER, WH ;

ROBLIN, RO .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1945, 67 (12) :2197-2200

[3]

BEIER N, 1994, HETEROCYCLES, V39, P117

[4] 6-ALKYL AND 5,6-DIALKYL-2-METHOXY-4(3H)-PYRIMIDINONES IN THE TRANSFORMATIONS OF PYRIMIDINES .2. SYNTHESIS AND CONVERSION INTO ALKYLURACILS AND 2-ALKOXY-4(3H)-PYRIMIDINONES [J].

BOTTA, M ;

CAVALIERI, M ;

CECI, D ;

DEANGELIS, F ;

FINIZIA, G ;

NICOLETTI, R .

TETRAHEDRON, 1984, 40 (17) :3313-3320

[5] THE PREPARATION OF FUSED TRIAZOLE SYSTEMS [J].

BOWER, JD ;

DOYLE, FP .

JOURNAL OF THE CHEMICAL SOCIETY, 1957, (FEB) :727-732

[6] ISOMERIZATIONS AKIN TO THE DIMROTH REARRANGEMENT .5. BIS-S-TRIAZOLO[4,3-A-4',3'-C]PYRIMIDINES AND RELATED SYSTEMS [J].

BROWN, DJ ;

NAGAMATSU, T .

AUSTRALIAN JOURNAL OF CHEMISTRY, 1979, 32 (07) :1585-1593

[7] SIMPLE PYRIMIDINES .2. 1-2-DIHYDRO-1-METHYLPYRIMIDINES AND THE CONFIGURATION OF THE N-METHYLURACILS [J].

BROWN, DJ ;

HOERGER, E ;

MASON, SF .

JOURNAL OF THE CHEMICAL SOCIETY, 1955, :211-217

[8]

BURCKHALTER JH, 1955, J AM PHARM ASS SC ED, V44, P515

[9]

CAMERINO B, 1960, GAZZ CHIM ITAL, V90, P1830

[10] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF A SERIES OF N-(BIPHENYLYLMETHYL)IMIDAZOLES AS POTENT, ORALLY ACTIVE ANTIHYPERTENSIVES [J].

CARINI, DJ ;

DUNCIA, JV ;

ALDRICH, PE ;

CHIU, AT ;

JOHNSON, AL ;

PIERCE, ME ;

PRICE, WA ;

SANTELLA, JB ;

WELLS, GJ ;

WEXLER, RR ;

WONG, PC ;

YOO, SE ;

TIMMERMANS, PBMWM .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2525-2547