Analogues of Thiolactomycin as Potential Antimalarial Agents

Analogues of the natural antibiotic thiolactomycin (TLM), an inhibitor of the condensing reactions of type II fatty acid synthase, were synthesized and evaluated for their ability to inhibit the growth of the malaria parasite Plasmodium falciparum. Alkylation of the C4 hydroxyl group led to the most...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-09, Vol.48 (19), p.5932-5941
Hauptverfasser:	Jones, Simon M, Urch, Jonathan E, Kaiser, Marcel, Brun, Reto, Harwood, John L, Berry, Colin, Gilbert, Ian H
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Oxoacyl-(Acyl-Carrier-Protein) Synthase - antagonists & inhibitors 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase - chemistry 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase - genetics Acetyltransferases - antagonists & inhibitors Acetyltransferases - chemistry Acetyltransferases - genetics Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Biological and medical sciences Cell Line Fatty Acid Synthase, Type II Isoenzymes - antagonists & inhibitors Isoenzymes - chemistry Isoenzymes - genetics Leishmania donovani Medical sciences Multienzyme Complexes - antagonists & inhibitors Multienzyme Complexes - chemistry Multienzyme Complexes - genetics Myoblasts - drug effects Myoblasts - parasitology Pharmacology. Drug treatments Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Rats Structure-Activity Relationship Thiophenes - chemical synthesis Thiophenes - chemistry Thiophenes - pharmacology Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi
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