Synthesis and Antitumor and Antibacterial Activity of Novel Dihydronaphthaline and Dihydrobenzo[H]Quinazoline Derivatives

被引：4

作者：

Markosyan, A. I. ^{[1
]}

Airapetyan, K. K. ^{[1
]}

Gabrielyan, S. A. ^{[1
]}

Mamyan, S. S. ^{[1
]}

Shirinyan, V. Z. ^{[2
]}

Zakharov, A. V. ^{[2
]}

Arsenyan, F. G. ^{[1
]}

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

Stepanyan, G. M. ^{[1
]}

机构：

[1] Natl Acad Sci Republ Armenia, AL Mndzhoyan Inst Fine Organ Chem, Sci Technol Ctr Organ & Pharmaceut Chem, 26 Azatutyan Prospekt, Erevan 0014, Armenia

[2] Russian Acad Sci, ND Zelinskii Inst Organ Chem, 47 Lenin Prospekt, Moscow 119991, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2019年 / 53卷 / 01期

基金：

俄罗斯基础研究基金会;

关键词：

cyclization; aminonitrile; benzo[h]quinazoline; antitumor and antibacterial activity; INHIBITORS;

D O I：

10.1007/s11094-019-01948-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A method for the synthesis of 1-amino-3,3-dimethyl-3,4-dihydronaphthaline-2-carbonitrile (-aminonitrile) was developed and used to synthesize Schiff bases, thioureide and chloracetamide derivatives. This latter was cyclized to 5,5-dimethyl-2-chloromethyl-5,6-dihydrobenzo[h]quinazoline-4(3H)-one, which was used to synthesize a series of 2-sulfanylmethyl and 2-aminomethyl derivatives. 2-Chloromethylbenzo[h]quinazoline in the presence of a base was found to form condensed heterocyclic compounds with seven rings: 1,1,11,11-tetramethyl-1,2,11,12-tetrahydropyrazino[2,1-b:5,4-b]di(benzo[h]quinazoline)-10,16(8H,18H)-di one. The antitumor properties of the compounds synthesized here were studied in an ascites carcinoma model and the antibacterial properties were studied using the agar diffusion method.

引用

页码：15 / 22

页数：8

共 21 条

[1] Synthesis and reactions of some new substituted pyridine and pyrimidine derivatives as analgesic, anticonvulsant and antiparkinsonian agents [J].