Synthesis of diphenoxyadamantane alkylamines with pharmacological interest
Georgiadis MO, Kourbeli V, Ioannidou V, Karakitsios E, Papanastasiou I, Tsotinis A, Komiotis D, Vocat A, et al. (11 authors)
Bioorganic & medicinal chemistry letters · 2019-04
Abstract
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.
MeSH terms
- Trypanosoma brucei brucei
- Mycobacterium tuberculosis
- Amines
- Adamantane
- Antitubercular Agents
- Trypanocidal Agents
- Parasitic Sensitivity Tests
- Molecular Structure
- Structure-Activity Relationship
- Dose-Response Relationship, Drug