SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF MERIBENDAN AND RELATED HETEROCYCLIC BENZIMIDAZOLO-PYRIDAZINONES

被引：67

作者：

JONAS, R ^{[1
]}

KLOCKOW, M ^{[1
]}

LUES, I ^{[1
]}

PRUCHER, H ^{[1
]}

SCHLIEP, HJ ^{[1
]}

WURZIGER, H ^{[1
]}

机构：

[1] E MERCK AG,PRECLIN PHARMACEUT RES LABS,FRANKFURTER STR 250,W-6100 DARMSTADT,GERMANY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 28卷 / 02期

关键词：

BENZIMIDAZOLE; CALCIUM SENSITIVITY; CARDIOTONICS; INOTROPES; PHOSPHODIESTERASE; PAPILLARY MUSCLE; PYRIDAZINONE;

D O I：

10.1016/0223-5234(93)90005-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of new heterocyclic benzimidazolo-pyridazinones is described. The new compounds were evaluated as inotropic agents with 'calcium-sensitizing' effects. 5-Methyl-6-[2-(3-pyrazolyl)-5-benzimidazolyl]-2,3,4,5-tetrahydro-pyridazin-3-one hydrochloride (meribendan) turned out to be the most interesting compound and was chosen for development as a positive inotrope.

引用

页码：129 / 140

页数：12

共 54 条

[31]

MANNSCHRECK A, 1985, KONTAKTE DARMSTADT, V1, P40

[32] GENERAL SYNTHESIS OF 3-(SUBSTITUTED BENZOYL)-3-SUBSTITUTED ALKANOIC ACIDS [J].

MCEVOY, FJ ;

ALLEN, GR .

JOURNAL OF ORGANIC CHEMISTRY, 1973, 38 (23) :4044-4048

[33] NONSTEROIDAL CARDIOTONICS .3. NEW 4,5-DIHYDRO-6-(1H-INDOL-5-YL)PYRIDAZIN-3(2H)-ONES AND RELATED-COMPOUNDS WITH POSITIVE INOTROPIC ACTIVITIES [J].

MERTENS, A ;

FRIEBE, WG ;

MULLERBECKMANN, B ;

KAMPE, W ;

KLING, L ;

VONDERSAAL, W .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (10) :2870-2875

[34] CARDIOTONIC AGENTS .8. SELECTIVE INHIBITORS OF ADENOSINE 3',5'-CYCLIC PHOSPHATE PHOSPHODIESTERASE-III - ELABORATION OF A 5-POINT MODEL FOR POSITIVE INOTROPIC ACTIVITY [J].

MOOS, WH ;

HUMBLET, CC ;

SIRCAR, I ;

RITHNER, C ;

WEISHAAR, RE ;

BRISTOL, JA ;

MCPHAIL, AT .

JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (11) :1963-1972

[35]

MURAKAMI T, 1981, HETEROCYCLES, V15, P301

[36] A NOVEL CLASS OF CARDIOTONICS - SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF [4-(SUBSTITUTED-AMINO)PHENYL]PYRIDAZINONES AND RELATED DERIVATIVES [J].

OKUSHIMA, H ;

NARIMATSU, A ;

KOBAYASHI, M ;

FURUYA, R ;

TSUDA, K ;

KITADA, Y .

JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (07) :1157-1161

[37]

OPIE LH, 1986, LANCET, V1, P1336

[38] AN ENANTIOSELECTIVE SYNTHESIS OF SK-AND-F-93505, A KEY INTERMEDIATE FOR PREPARING CARDIOTONIC AGENTS [J].

OWINGS, FF ;

FOX, M ;

KOWALSKI, CJ ;

BAINE, NH .

JOURNAL OF ORGANIC CHEMISTRY, 1991, 56 (05) :1963-1966

[39]

PIMOBENDAN, 1989, DRUGS FUTURE, V14, P713

[40]

RAKHIT S, 1986, EUR J MED CHEM, V21, P511

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