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

Socpus ID

38149038655 (Scopus)

Source API URL

https://api.elsevier.com/content/abstract/scopus_id/38149038655

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