In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine

doi:10.1016/j.bmcl.2005.04.036

Bioorganic & Medicinal Chemistry Letters

Volume 15, Issue 12, 15 June 2005, Pages 2974-2979

https://doi.org/10.1016/j.bmcl.2005.04.036 Get rights and content

Abstract

The preparation and biological activity of analogs of (−)-cytisine, an α4β2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (−)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (−)-cytisine.

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In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine

Abstract

Graphical abstract

Curr. Drug Targets—CNS Neurol. Disord.

Eur. J. Neurosci.

J. Theor. Biol.

J. Pharmacol. Exp. Ther.

J. Clin. Psychiatry Monograph

Dtsch. Gesundheitsw.

Org. Lett.

Farmaco

Farmaco

J. Am. Chem. Soc.

Synthesis

Bull. World Health Organ.

Tob Control.

BMJ

BMJ

Ann. Rev. Med.

Engl. J. Med.

Drugs

Drug Disc. Today

BMJ

J. Psychoactive Drugs

Eur. J. Pharmacol.

Psychopharmacology

Pharmacol. Biochem. Behav.

Nature

Pharmacol. Biochem. Behav.

Science

Neuropharmacology

Mol. Pharmacol.