SYNTHESIS AND DOPAMINE ANTAGONIST ACTIVITY OF 2-THIOETHER DERIVATIVES OF THE ERGOLINE RING-SYSTEM

被引：14

作者：

TUPPER, DE ^{[1
]}

PULLAR, IA ^{[1
]}

CLEMENS, JA ^{[1
]}

FAIRHURST, J ^{[1
]}

RISIUS, FC ^{[1
]}

TIMMS, GH ^{[1
]}

WEDLEY, S ^{[1
]}

机构：

[1] ELI LILLY & CO,LILLY RES LAB,LILLY CORP CTR,INDIANAPOLIS,IN 46285

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 07期

关键词：

D O I：

10.1021/jm00059a017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-thioether derivatives of a number of clavine alkaloid (ergoline) ring systems have been synthesized and tested for dopamine antagonist activity. Of the compounds tested 2-(methylthio)-agroclavine (8,9-didehydro-6,8-dimethyl-2-(methylthio)ergoline) (6) was the most potent and had a profile of activity in animal models indicative of potential antipsychotic activity. The synthesis and biological activity of a number of metabolites of 6, including the 13-hydroxy derivative, are also reported.

引用

页码：912 / 918

页数：7

共 36 条

[1] ABE M, 1948, J AGR CHEM SOC JPN, V22, P61
[2] BICYCLIC AND TRICYCLIC ERGOLINE PARTIAL STRUCTURES - RIGID 3-(2-AMINOETHYL)PYRROLES AND 3-(2-AMINOETHYL)PYRAZOLE AND 4-(2-AMINOETHYL)PYRAZOLE AS DOPAMINE AGONISTS
BACH, NJ
KORNFELD, EC
JONES, ND
CHANEY, MO
DORMAN, DE
PASCHAL, JW
CLEMENS, JA
SMALSTIG, EB
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1980, 23 (05) : 481 - 491
[3] BARGER G, 1906, BRIT MED J, V2, P1792
[4] BROMOCRIPTINE ALONE OR ASSOCIATED WITH L-DOPA PLUS BENSERAZIDE IN PARKINSONS-DISEASE
CARACENI, TA
CELANO, I
PARATI, E
GIROTTI, F
[J]. JOURNAL OF NEUROLOGY NEUROSURGERY AND PSYCHIATRY, 1977, 40 (12) : 1142 - 1146
[5] CARLSSON A, 1970, AMPHETAMINES RELATED, P289
[6] CORUM CJ, COMMUNICATION
[7] CHOLINERGIC-INDUCED AND NEUROLEPTIC-INDUCED CATALEPSY - MODIFICATION BY LESIONS IN CAUDATE-PUTAMEN
COSTALL, B
OLLEY, JE
[J]. NEUROPHARMACOLOGY, 1971, 10 (03) : 297 - &
[8] DOPAMINE RECEPTOR-BINDING PREDICTS CLINICAL AND PHARMACOLOGICAL POTENCIES OF ANTI-SCHIZOPHRENIC DRUGS
CREESE, I
BURT, DR
SNYDER, SH
[J]. SCIENCE, 1976, 192 (4238) : 481 - 483
[9] ERGOT ALKALOIDS - SYNTHESIS OF 6-ALKYL-8-ERGOLENES AND 6-METHYL-8-AMINOERGOLINES AS POTENTIAL PROLACTIN INHIBITORS
CRIDER, AM
ROBINSON, JM
FLOSS, HG
CASSADY, JM
CLEMENS, JA
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1977, 20 (11) : 1473 - 1477
[10] DEMAIO D, 1972, ARZNEI-FORSCHUNG, V22, P919

← 1 2 3 4 →