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Design and Synthesis of Trypanosoma brucei Active 1‐Alkyloxy and 1‐Benzyloxyadamantano 2‐Guanylhydrazones |
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| Authors: | Ioannis Papanastasiou Dr. Andrew Tsotinis Prof. Grigoris Zoidis Dr. Nicolas Kolocouris Prof. S. Radhika Prathalingam Dr. John M. Kelly Prof. |
| Affiliation: | 1. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli‐Zografou, 157 71 Athens (Greece), Fax.: (+30)?210‐7274747;2. Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London WC1E 7HT (UK), Fax.: (+44)?207‐636‐8739 |
| Abstract: | Treating African trypanosomiasis : The synthesis and biological evaluation of novel 1‐alkyloxy and 1‐benzyloxyadamantano 2‐guanylhydrazones, their 1‐dioxa congeners and two 1‐benzyladamantano 2‐guanylhydrazones is reported. Preliminary structure–activity relationship data were elucidated and lead compounds suitable for further optimization were discovered.  |
| Keywords: | guanylhydrazones drug design structure– activity relationships antiparasitic agents trypanocidal action |