SYNTHESIS, PHYSICOCHEMICAL AND CONFORMATIONAL PROPERTIES OF (3R,4R)-3-(3-CYCLOPROPYL-1,2,4-OXADIAZOL-5-YL)-1-AZABICYCLO[2.2.1]HEPTANE, A NOVEL M(1) SELECTIVE MUSCARINIC PARTIAL AGONIST

被引：11

作者：

BAKER, R

SHOWELL, GA

STREET, LJ

SAUNDERS, J

HOOGSTEEN, K

FREEDMAN, SB

HARGREAVES, RJ

机构：

[1] MERCK SHARP & DOHME LTD,DEPT BIOCHEM,HARLOW CM20 2QR,ESSEX,ENGLAND

[2] MERCK SHARP & DOHME LTD,RAHWAY,NJ 07065

[3] MERCK SHARP & DOHME LTD,DEPT PHARMACOL,HARLOW CM20 2QR,ESSEX,ENGLAND

来源：

JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS | 1992年 / 11期

关键词：

D O I：

10.1039/c39920000817

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The cyclopropyloxadiazole derivative described in the title has been shown to be a functionally selective M1 partial agonist with antagonist properties in M2 and M3 muscarinic receptor assays; conformational studies indicate free rotation around the oxadiazole-azanorbornane bond, whilst X-ray studies reveal that the cyclopropyl group is in conjugation with the oxadiazole C=N bond.

引用

页码：817 / 819

页数：3

共 16 条

[1] IDENTIFICATION OF A FAMILY OF MUSCARINIC ACETYLCHOLINE-RECEPTOR GENES
BONNER, TI
BUCKLEY, NJ
YOUNG, AC
BRANN, MR
[J]. SCIENCE, 1987, 237 (4814) : 527 - 532
[2] A SYNTHESIS OF 1-AZABICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID-ESTERS IN ENANTIOMERICALLY PURE FORM
COTTRELL, IF
HANDS, D
KENNEDY, DJ
PAUL, KJ
WRIGHT, SHB
HOOGSTEEN, K
[J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1991, (05): : 1091 - 1097
[3] RECENT RESEARCH ON THE CAUSES OF ALZHEIMERS-DISEASE - WHAT CAUSES NEURONAL DEATH, AND WHY THE SPECIFIC PATTERNS
DEARY, IJ
WHALLEY, LJ
[J]. BRITISH MEDICAL JOURNAL, 1988, 297 (6652) : 807 - 810
[4] THE DEVELOPMENT AND USE OF QUANTUM-MECHANICAL MOLECULAR-MODELS .76. AM1 - A NEW GENERAL-PURPOSE QUANTUM-MECHANICAL MOLECULAR-MODEL
DEWAR, MJS
ZOEBISCH, EG
HEALY, EF
STEWART, JJP
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1985, 107 (13) : 3902 - 3909
[5] NEUROPHARMACOLOGY OF DEGENERATIVE DISEASES ASSOCIATED WITH AGING
GROWDON, JH
[J]. MEDICINAL RESEARCH REVIEWS, 1983, 3 (03) : 237 - 257
[6] MUSCARINIC RECEPTOR SUBTYPES - M1 AND M2 BIOCHEMICAL AND FUNCTIONAL-CHARACTERIZATION
HAMMER, R
GIACHETTI, A
[J]. LIFE SCIENCES, 1982, 31 (26) : 2991 - 2998
[7] DRUG DEVELOPMENT FOR SENILE COGNITIVE DECLINE
HERSHENSON, FM
MOOS, WH
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (07) : 1125 - 1130
[8] CHOLINERGIC APPROACHES TO THE TREATMENT OF ALZHEIMERS-DISEASE
HOLLANDER, E
MOHS, RC
DAVIS, KL
[J]. BRITISH MEDICAL BULLETIN, 1986, 42 (01) : 97 - 100
[9] IVERSEN S, 1988, CHEM BR, P338
[10] DISTINCT PRIMARY STRUCTURES, LIGAND-BINDING PROPERTIES AND TISSUE-SPECIFIC EXPRESSION OF 4 HUMAN MUSCARINIC ACETYLCHOLINE-RECEPTORS
PERALTA, EG
ASHKENAZI, A
WINSLOW, JW
SMITH, DH
RAMACHANDRAN, J
CAPON, DJ
[J]. EMBO JOURNAL, 1987, 6 (13) : 3923 - 3929

← 1 2 →