SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency

Syntheses of a variety of new analogues of cocaine are reported together with their binding affinities and dopamine uptake inhibition activities. The present work further expands the SAR data base for cocaine. Further structural modifications to cocaine are reported together with the results of bind...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 3; no. 6; pp. 1327 - 1332
Main Authors Kozikowski, Alan P., Roberti, Marinella, Johnson, Kenneth M., Bergmann, John S., Ball, Richard G.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.06.1993
Online AccessGet full text

Cover

More Information
Summary:Syntheses of a variety of new analogues of cocaine are reported together with their binding affinities and dopamine uptake inhibition activities. The present work further expands the SAR data base for cocaine. Further structural modifications to cocaine are reported together with the results of binding experiments and dopamine uptake inhibition studies. Compound 5 was found to possess subnanomolar binding affinity for the cocaine recognition site.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)80341-8