Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives

被引：27

作者：

Kubota, H

Rothman, RB

Dersch, C

McCullough, K

Pinto, J

Rice, KC

机构：

[1] NIDDK, Med Chem Lab, NIH, Bethesda, MD 20892 USA

[2] NIDA, Addict Res Ctr, Clin Psychopharmacol Sect, Baltimore, MD 21224 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00105-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 3-unsubstituted and substituted analogs of naltrindole (NTI) were synthesized using palladium-catalyzed transformations, and their binding affinity to opioid receptors was determined. Although the 3-desoxy analog showed comparable delta selectivity with that of NTI, all of the novel compounds possessed low affinity for delta receptors indicating the important role of the 3-oxygen atom of NTI for interaction with delta-opioid receptors. Published by Elsevier Science Ltd.

引用

页码：799 / 804

页数：6

共 30 条

[1]

ABDELHAMID EE, 1991, J PHARMACOL EXP THER, V258, P299

[2]

CHAVKIN C, 1981, P NATL ACAD SCI USA, V78, P6453

[3]

CHENG PY, 1993, EUR J PHARMACOL, V267, P852

[4]

COWAN A, 1988, J PHARMACOL EXP THER, V246, P950