Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.

JOhkanda; JWLockman; KYokoyama; MHGelb; SL Croft ORCID logo; HKendrick; MIHarrell; JEFeagin; MABlaskovich; SMSebti; +1 more... ADHamilton; (2001) Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity. Bioorganic & medicinal chemistry letters, 11 (6). pp. 761-764. ISSN 0960-894X DOI: 10.1016/s0960-894x(01)00055-5
Copy

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 paper we report the design, synthesis, and evaluation of potential antimalarial agents against a novel target, protein farnesyltransferase. We show that the most potent compounds are active against Plasmodium falciparum in vitro at submicromolar concentrations.
Item Type Article
Keywords Discovery, targets, enzyme, Alkyl and Aryl Transferases, antagonists & inhibitors, metabolism, Animal, Antimalarials, chemical synthesis, chemistry, pharmacology, Drug Design, Drug Resistance, Enzyme Inhibitors, chemical synthesis, chemistry, pharmacology, Imidazoles, chemical synthesis, chemistry, pharmacology, Inhibitory Concentration 50, Parasitic Sensitivity Tests, Plasmodium falciparum, drug effects, Structure-Activity Relationship, Support, Non-U.S. Gov't, Support, U.S. Gov't, P.H.S.
ISI 167571100003

Atom BibTeX OpenURL ContextObject in Span Multiline CSV OpenURL ContextObject Dublin Core Dublin Core MPEG-21 DIDL EndNote HTML Citation JSON MARC (ASCII) MARC (ISO 2709) METS MODS RDF+N3 RDF+N-Triples RDF+XML RIOXX2 XML Reference Manager Refer Simple Metadata ASCII Citation EP3 XML
Export

Downloads

Full text not available from this repository.

Explore Further

Read more research from the creator(s):

Find work associated with the faculties and division(s):

Find work associated with the research centre(s):

Find work from this publication: