Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity |
| |
| Authors: | Kettler Katja Wiesner Jochen Silber Katrin Haebel Peter Ortmann Regina Sattler Isabel Dahse Hans-Martin Jomaa Hassan Klebe Gerhard Schlitzer Martin |
| |
| Affiliation: | Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians Universit?t München, Butenandtstrasse 5-13, 81377 München, Germany. |
| |
| Abstract: | ![]()
Water solubility was previously found to be essential for in vivo-antimalarial activity of a novel type of benzophenone-based farnesyltransferase inhibitors. Introduction of a alpha-amino group into the phenylacetic acid substructure provided more soluble compounds with high farnesyltransferase inhibitory activity. The in vitro-antimalarial activity was detrimentally influenced by this structural modification. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
