Design and synthesis of new adamantyl-substituted antileishmanial ether phospholipids |
| |
| Authors: | Ioannis Papanastasiou Kyriakos C. Prousis Kalliopi Georgikopoulou Theofilos Pavlidis Effie Scoulica Nicolas Kolocouris Theodora Calogeropoulou |
| |
| Affiliation: | 1. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli-Zografou, Athens 15771, Greece;2. Institute of Organic and Pharmaceutical Chemistry, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, Athens 11635, Greece;3. Department of Clinical Bacteriology, Parasitology, Zoonoses and Geographical Medicine, School of Medicine, University of Crete, Heraklion 71409, Greece |
| |
| Abstract: | A series of new 2-[3-(2-alkyloxy-ethyl)-adamantan-1-yl]-ethoxy substituted ether phospholipids was synthesized and their antileishmanial activity was evaluated against Leishmania infantum amastigotes. The majority of the new analogues were significantly less cytotoxic than miltefosine while, antiparasitic activity depended on the length of the 2-alkyloxy substituent. The most potent compounds were {2-[[[3-(2-hexyloxy-ethyl)-adamant-1-yl]-ethoxy]hydroxyphosphinyloxy]ethyl}-Ν,Ν,Ν-trimethyl-ammonium inner salt (5b) and {2-[[[3-(2-octyloxy-ethyl)-adamant-1-yl]-ethoxy]hydroxyphosphinyloxy]ethyl}-Ν,Ν,Ν-trimethyl-ammonium inner salt (5c). |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
