SYNTHESIS AND PRELIMINARY BIOLOGICAL STUDIES OF 4-[2-HYDROXY-3-(ISOPROPYLAMINO)PROPOXY]BENZIMIDAZOLES AND 5-[2-HYDROXY-3-(ISOPROPYLAMINO)PROPOXY]BENZIMIDAZOLES - SELECTIVE BETA-2 ADRENERGIC BLOCKING-AGENTS

被引：10

作者：

CROOKS, CR ^{[1
]}

WRIGHT, J ^{[1
]}

CALLERY, PS ^{[1
]}

MORETON, JE ^{[1
]}

机构：

[1] UNIV MARYLAND, SCH PHARM, DEPT MED CHEM, BALTIMORE, MD 21201 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 02期

关键词：

D O I：

10.1021/jm00188a019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Benzimidazoles carrying the 2-hydroxy-3-(isopropylamino)propoxy side chain at either the C-4 or C-5 ring positions were synthesized and investigated for .beta.-adrenergic blocking activity. Both compounds demonstrated .beta.2 selectivity when evaluated in guinea pig atrial and tracheal preparations. The C-4 isomer was 17 times more selective toward tracheal tissue, and its overall potency was roughly comparable to that of propranolol. .beta.2 selectivity of the C-5 isomer was minimal, with a potency about 1/100 that of propranolol.

引用

页码：210 / 213

页数：4

共 35 条

[31] CARDIOVASCULAR STUDIES OF 5-(3-TERT-BUTYLAMINO-2-HYDROXY) PROPOXY-3,4-DIHYDROCARBOSTYRIL HYDROCHLORIDE (OPC-1085), A NEW POTENT BETA-ADRENERGIC BLOCKING-AGENT
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KINOSHITA, D
[J]. JAPANESE JOURNAL OF PHARMACOLOGY, 1974, 24 (06) : 853 - 861
[32] SYNTHESIS AND BIOLOGICAL-ACTIVITY OF DL-3-(5-BENZIMIDAZOLYL)-2-METHYLALANINE
ZENKER, N
MORGENRO.VH
WRIGHT, J
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1974, 17 (11) : 1223 - 1225
[33] 1970, Patent No. 1543690
[34] 1969, PHARMACOLOGICAL EXPT, P306
[35] 1969, PHARMACOLOGICAL EXPT, P100

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