Syntheses and radioligand activities of dimebon analogs

Several analogs of the antihistamine drug dimebon have been synthesized with different linkers connecting a picoline fragment to the tetrahydropyridoindole core. Radioligand activity profiles of the obtained compounds have been studied using a broad set of 30 therapeutic targets. Reduction of the li...

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Bibliographic Details
Published inPharmaceutical chemistry journal Vol. 45; no. 9; pp. 526 - 531
Main Authors Ivashchenko, A. V., Mit’kin, O. D., Okun’, I. M., Kuznetsova, I. V.
Format Journal Article
LanguageEnglish
Published Boston Springer US 01.12.2011
Springer
Subjects
Antihistamines
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
synthesis
linkers
activity
receptors
activity profile
analogs
dimebon
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Summary:Several analogs of the antihistamine drug dimebon have been synthesized with different linkers connecting a picoline fragment to the tetrahydropyridoindole core. Radioligand activity profiles of the obtained compounds have been studied using a broad set of 30 therapeutic targets. Reduction of the linker length is shown to cause substantial shifts in the activity profiles.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-011-0672-1