Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

Authors
Ohkanda, J Lockman, JW Yokoyama, K Gelb, MH Croft, SL Kendrick, H Harrell, MI Feagin, JE Blaskovich, MA Sebti, SM Hamilton, AD
Citation
J. Ohkanda et al., Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity, BIOORG MED, 11(6), 2001, pp. 761-764
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
6
Year of publication
2001
Pages
761 - 764
Database
ISI
SICI code
0960-894X(20010326)11:6<761:PIOPFS>2.0.ZU;2-E
Abstract
Malaria continues to represent a very serious health problem in the tropics . The current methods of clinical treatment are showing deficiencies due to the increased incidence of resistance in the parasite. In the present pape r we report the design, synthesis, and evaluation of potential antimalarial agents against a novel target, protein farnesyltransferase. We show that t he most potent compounds are active against Plasmodium falciparum in vitro at submicromolar concentrations. (C) 2001 Elsevier Science Ltd. All rights reserved.