SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-(4-SUBSTITUTED PHENYL)-1-ALKYL(ARYL)-2-PHENYL-3-AMINOPROPAN-1-OL HYDROCHLORIDES

被引：0

作者：

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

Mardanyan, S. S. ^{[2
]}

Vermishyan, I. G. ^{[2
]}

Antonyan, A. A. ^{[2
]}

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

Panosyan, G. A. ^{[3
]}

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

机构：

[1] Natl Acad Sci Republ Armenia, Sci Tech Ctr Organ & Pharmaceut Chem, AL Mndzhoyan Inst Fine Organ Chem, Erevan 0014, Armenia

[2] Natl Acad Sci Republ Armenia, G Kh Bunyatyan Inst Biochem, Erevan 0014, Armenia

[3] Natl Acad Sci Republ Armenia, Ctr Study Mol Struct, Erevan 0014, Armenia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2015年 / 49卷 / 05期

关键词：

aminopropiophenones; aminomethylation; aminopropan-1-ols; adenosine deaminase (ADA) inhibitors; ADENOSINE-DEAMINASE ACTIVITY; PURIFICATION; DEFICIENCY; INHIBITORS; BINDING; PROTEIN; DISEASE; ANALOGS; BRAIN; RAT;

D O I：

10.1007/s11094-015-1276-y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1-(4-Substituted phenyl)-2-phenylethanones were aminomethylated with paraformaldehyde and amine in ethanol to produce alpha-phenyl-beta-amino-4-substituted propiophenones. Interaction of these with Grignard reagents in ether yielded tertiary aminopropan-1-ols and their hydrochlorides. Quite efficient inhibition, at differing levels, of adenosine deaminase (ADA, E.C. 3.5.44), one of the key enzymes in purine metabolism, by the compounds synthesized here was demonstrated. A structure-activity relationship was found for ADA inhibition. Most of the compounds synthesized here were found to lack antibacterial activity; only compounds Va, Vd, and VId displayed moderate levels of antibacterial activity against Gram-positive microorganisms.

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页码：313 / 318

页数：6

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