Radiosynthesis and biological evaluation of a novel enoyl-ACP reductase inhibitor for Staphylococcus aureus
نویسندگان
چکیده
منابع مشابه
A slow, tight-binding inhibitor of InhA, the enoyl-ACP reductase from Mycobacterium tuberculosis
InhA, the enoyl-ACP reductase in Mycobacterium tuberculosis is an attractive target for the development of novel drugs against tuberculosis, a disease that kills more than two million people each year. InhA is the target of the current first line drug isoniazid (INH) for the treatment of tuberculosis infections. Compounds that directly target InhA and do not require activation by the mycobacter...
متن کاملIn silico screening for Plasmodium falciparum enoyl-ACP reductase inhibitors
The need for novel therapeutics against Plasmodium falciparum is urgent due to recent emergence of multi-drug resistant malaria parasites. Since fatty acids are essential for both the liver and blood stages of the malarial parasite, targeting fatty acid biosynthesis is a promising strategy for combatting P. falciparum. We present a combined computational and experimental study to identify novel...
متن کاملIdentification of flavonoid with potential for inhibitor Enoyl-ACP Reductase in Plasmodium falciparum by hierarquical virtual screening
Malaria is a parasitic infection and is considered a serious global public health problem [1]. Plasmodium falciparum provides easy adaptability by mutation, causing resistance to antimalarials [2]. This study aimed to search antimalarial potential showed by some flavonoids to inhibit promising target, enoyl-ACP reductase (PfENR), present in limiting step in the biosynthesis of fatty acids type ...
متن کاملFunctional, thermodynamics, structural and biological studies of in silico-identified inhibitors of Mycobacterium tuberculosis enoyl-ACP(CoA) reductase enzyme
Novel chemotherapeutics agents are needed to kill Mycobacterium tuberculosis, the main causative agent of tuberculosis (TB). The M. tuberculosis 2-trans-enoyl-ACP(CoA) reductase enzyme (MtInhA) is the druggable bona fide target of isoniazid. New chemotypes were previously identified by two in silico approaches as potential ligands to MtInhA. The inhibition mode was determined by steady-state ki...
متن کاملMechanism and inhibition of the FabI enoyl-ACP reductase from Burkholderia pseudomallei.
OBJECTIVES As an initial step in developing novel antibacterials against Burkholderia pseudomallei, we have characterized the FabI enoyl-ACP reductase homologues in the type II fatty acid biosynthesis pathway from this organism and performed an initial enzyme inhibition study. METHODS A BLAST analysis identified two FabI enoyl-ACP reductase homologues, bpmFabI-1 and bpmFabI-2, in the B. pseud...
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2014
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2014.09.008