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Synthesis and structure-activity data of some new epibatidine analogues.

Abstract：

:The high-pressure Diels-Alder reaction of N-carbomethyoxypyrroles and phenyl vinyl sulfone affords versatile intermediates for the palladium-catalyzed preparation of new epibatidine analogues. Structure-activity relationships of new epibatidine analogues are presented. High affinities of Ki = 0.81 and 2.6 nM for the [3H]-cytisine rat brain nicotinic acetylcholine binding sites were found for the 5-pyrimidinyl and the 5-(2-amino)-pyrimidinyl epibatidine analogues, respectively.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Seerden JP,Tulp MT,Scheeren HW,Kruse CG

doi

10.1016/s0968-0896(98)00163-1

subject

Has Abstract

pub_date

1998-11-01 00:00:00

pages

2103-10

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968089698001631

journal_volume

6

pub_type

杂志文章

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