Title
2-Oxo-Tetrahydro-1,8-Naphthyridines As Selective Inhibitors Of Malarial Protein Farnesyltransferase And As Anti-Malarials
Keywords
Anti-malarials; Drug discovery; Malaria; P. falciparum; Protein farnesyltransferase; Rational drug design
Abstract
A new class of 2-oxo-tetrahydro-1,8-naphthyridine-based protein farnesyltransferase inhibitors were synthesized and found to inhibit protein farnesyltransferase from the malaria parasite with potencies in the low nanomolar range. The compounds were much less potent on mammalian protein prenyltransferases. Two of the compounds block the growth of malaria in culture with potencies in the sub-micromolar range. Some of the compounds were found to be much more metabolically stable than previously described tetrahydroquinoline-based protein farnesyltransferase inhibitors. © 2007 Elsevier Ltd. All rights reserved.
Publication Date
1-15-2008
Publication Title
Bioorganic and Medicinal Chemistry Letters
Volume
18
Issue
2
Number of Pages
494-497
Document Type
Article
Personal Identifier
scopus
DOI Link
https://doi.org/10.1016/j.bmcl.2007.11.104
Copyright Status
Unknown
Socpus ID
38149038655 (Scopus)
Source API URL
https://api.elsevier.com/content/abstract/scopus_id/38149038655
STARS Citation
Olepu, Srinivas; Suryadevara, Praveen Kumar; Rivas, Kasey; Yokoyama, Kohei; and Verlinde, Christophe L.M.J., "2-Oxo-Tetrahydro-1,8-Naphthyridines As Selective Inhibitors Of Malarial Protein Farnesyltransferase And As Anti-Malarials" (2008). Scopus Export 2000s. 10577.
https://stars.library.ucf.edu/scopus2000/10577