SYNTHESIS AND BIOLOGICAL PROPERTIES OF 2-(4-CHLOROPHENYL)-3-MORPHOLIN-4-YL-(4-ALKOXYPHENYL)ALKANOL HYDROCHLORIDES

被引：2

作者：

Papoyan, O. A. ^{[1
]}

Gasparyan, N. K. ^{[1
]}

Paronikyan, R. G. ^{[1
]}

Tatevosyan, A. A. ^{[1
]}

Avakimyan, D. A. ^{[1
]}

Panosyan, G. A. ^{[2
]}

Gevorgyan, G. A. ^{[1
]}

机构：

[1] Natl Acad Sci Armenia, AI Mndzhoyan Fine Organ Chem Inst, Sci & Technol Ctr Organ & Pharmaceut Chem, Yerevan 0014, Armenia

[2] Natl Acad Sci Armenia, Mol Struct Res Ctr, Yerevan 0014, Armenia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2011年 / 45卷 / 08期

关键词：

aminomethylation; 3-morpholinopropan-1-ones; Grignard reagents; 3-morpholinoalkan-1-ols; 1-morpholinoalkan-3-ols; anticonvulsive; peripheral n-cholinolytic properties; antibacterial activity;

D O I：

10.1007/s11094-011-0655-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New 2-(4-chlorophenyl)-3-morpholin-4-yl-1-(4-alkoxyphenyl)propan-1-ones were synthesized via amino-methylation of 2-(4-chlorophenyl)-1-(4-alkoxyphenyl)ethanones. Reduction of the former by lithium aluminum hydride produced 2-(4-chlorophenyl)-3-morpholin-4-yl-1-(4-alkoxyphenyl)propan-1-ols. Reaction of them with Grignard reagents gave 2-(4-chlorophenyl)-1-morpholin-4-yl-3-(4-alkoxyphenyl) alkan-3-ols. The synthesized compounds exhibited pronounced anticonvulsive and some peripheral n-cholinolytic activities while showing no antibacterial activity.

引用

页码：461 / 465

页数：5

共 9 条

[1] Belenkii M.L., 1963, Elements of quantitative assessment of pharmacological effect
[2] Gasparyan N. K., 2005, Khimiko-Farmatsevticheskii Zhurnal, V39, P23
[3] GEROLD M, 1966, ANTIBIOTICS, P93
[4] Gevorgyan G. A., 2009, ZH ORG KHIM, V45, P1854
[5] Gevorgyan G. A., 1971, ARM KHIM ZH, V24, P333
[6] GEVORGYAN GA, 2010, KHIM ZH ARMENII, V62, P354
[7] GEVORKYAN KA, 1987, KHIM FARM ZH+, V21, P167
[8] Kharkevich D. A., 1981, HDB PRACTICAL TASKS, P104
[9] PAPOYAN OA, 2010, KHIM ZH ARMENII, V62, P242

← 1 →