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Synthesis of diphenoxyadamantane alkylamines with pharmacological interest

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Autor
Georgiadis M.-O., Kourbeli V., Ioannidou V., Karakitsios E., Papanastasiou I., Tsotinis A., Komiotis D., Vocat A., Cole S.T., Taylor M.C., Kelly J.M.
Fecha
2019
Language
en
DOI
10.1016/j.bmcl.2019.04.010
Materia
aliphatic amine
antitrypanosomal agent
diphenoxyadamantane alkylamine
tuberculostatic agent
unclassified drug
adamantane
amine
antitrypanosomal agent
tuberculostatic agent
antibacterial activity
Article
bacterial growth
controlled study
drug structure
drug synthesis
growth inhibition
Mycobacterium tuberculosis
nonhuman
trypanocidal activity
Trypanosoma brucei
chemical structure
chemistry
dose response
drug effect
drug sensitivity
structure activity relation
synthesis
Trypanosoma brucei brucei
Adamantane
Amines
Antitubercular Agents
Dose-Response Relationship, Drug
Molecular Structure
Mycobacterium tuberculosis
Parasitic Sensitivity Tests
Structure-Activity Relationship
Trypanocidal Agents
Trypanosoma brucei brucei
Elsevier Ltd
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Resumen
In this work, the synthesis and the pharmacological evaluation of diphenoxyadamantane alkylamines Ia–f and IIa–f is described. The new diphenoxy-substituted adamantanes share structural features present in trypanocidal and antitubercular agents. 1-Methylpiperazine derivative Ia is the most potent against T. brucei compound, whilst its hexylamine congener IIf exhibits a significant antimycobacterial activity. © 2019 Elsevier Ltd
URI
http://hdl.handle.net/11615/72127
Colecciones
  • Δημοσιεύσεις σε περιοδικά, συνέδρια, κεφάλαια βιβλίων κλπ. [19735]

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