SYNTHESES AND BIOACTIVITIES OF 1-(HYDROXYPHENYL)-1-NONEN-3-ONES AND RELATED ETHERS AND ESTERS

被引：20

作者：

DIMMOCK, JR ^{[1
]}

NYATHI, CB ^{[1
]}

SMITH, PJ ^{[1
]}

机构：

[1] UNIV SASKATCHEWAN, DEPT CHEM & CHEM ENGN, SASKATOON S7N 0W0, SASKATCHEWAN, CANADA

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 10期

关键词：

Antineoplastic agents; potential—nuclear hydroxy styryl ketones; syntheses; structure‐activity relationships; Nuclear hydroxy styryl ketones—syntheses; antineoplastic activity; antimicrobial activity; analgesic activity; anti‐inflammatory activity; antianaphylactic activity; Structure‐activity relationships— hydroxy styryl ketones; antianaphyiactic activity;

D O I：

10.1002/jps.2600681006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of nuclear hydroxy styryl ketones and related compounds were prepared and evaluated for antineoplastic and antimicrobial activities as well as for analgesic, anti‐inflammatory, and antianaphylactic properties. The second‐order rate constants for the reaction of several esters with hydroxide ion in aqueous dioxane (50% v/v) at 36.9° were determined. The screening results showed that activity against P‐388 lymphocytic leukemia was found solely with the ethers and that antimicrobial properties were obtained virtually exclusively with the phenolic derivatives. All compounds showed analgesic properties, except for four that were algesic. While little anti‐inflammatory activity was found, several compounds showed some antianaphylaxis. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：1216 / 1221

页数：6

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