Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors

K I Choi; J H Cha; Y S Cho; A N Pae; C Jin; J Yook; H G Cheon; D Jeong; J Y Kong; H Y Koh

doi:10.1016/s0960-894x(99)00477-1

Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors

Bioorg Med Chem Lett. 1999 Oct 4;9(19):2795-800. doi: 10.1016/s0960-894x(99)00477-1.

Authors

K I Choi¹, J H Cha, Y S Cho, A N Pae, C Jin, J Yook, H G Cheon, D Jeong, J Y Kong, H Y Koh

Affiliation

¹ Life Sciences Division, Korea Institute of Science and Technology, Seoul.

PMID: 10522693
DOI: 10.1016/s0960-894x(99)00477-1

Abstract

A series of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles synthesized showed different binding characteristics to acetylcholine receptors depending on the substituents on the phenyl ring. Small polar substituents gave preferential binding affinity to nicotinic receptors, and large hydrophobic substituents to muscarinic receptors.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alkaloids / chemistry
Aza Compounds / chemistry*
Azocines
Binding, Competitive
Bridged Bicyclo Compounds, Heterocyclic / chemistry*
Isoxazoles / chemistry*
Molecular Structure
N-Methylscopolamine / chemistry
Protein Binding
Quinolizines
Receptors, Cholinergic / chemistry*
Receptors, Muscarinic / chemistry
Receptors, Nicotinic / chemistry

Substances

Alkaloids
Aza Compounds
Azocines
Bridged Bicyclo Compounds, Heterocyclic
Isoxazoles
Quinolizines
Receptors, Cholinergic
Receptors, Muscarinic
Receptors, Nicotinic
cytisine
N-Methylscopolamine