About: Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents

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About: Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents
Creator	Chibale, Kelly Smith, Peter D', Matthias De Kock, Carmen De Vreese, Rob
Source	PMC
abstract	AIM: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan-histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoform-selective HDACis. RESULTS: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity. CONCLUSION: Four hHDAC6 inhibitors showed submicromolar potency against both a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum with high selectivity indices, pointing to the relevance of exploring hHDAC6 inhibitors as potential new antiplasmodial agents.
has issue date	2017-03-06(xsd:dateTime)
bibo:doi	10.4155/fmc-2016-0215
bibo:pmid	28263085
has license	cc-by
sha1sum (hex)	aa128e608087f6902fd482e53d2c24b177b9f1e9
schema:url	https://doi.org/10.4155/fmc-2016-0215
resource representing a document's title	Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents
has PubMed Central identifier	PMC7099625
has PubMed identifier	28263085
schema:publication	Future Med Chem
resource representing a document's body	covid:aa128e608087f6902fd482e53d2c24b177b9f1e9#body_text
is schema:about of	named entity 'malaria' named entity 'falciparum' named entity 'powerful' named entity 'RESEARCH' named entity 'HISTONE DEACETYLASE INHIBITORS' named entity 'RESULTS' named entity 'PLASMODIUM FALCIPARUM' named entity 'CORRELATION' named entity 'DEPLOYMENT' covid:arg/aa128e608087f6902fd482e53d2c24b177b9f1e9 named entity 'antiplasmodial' named entity 'inhibitors' named entity 'The' named entity 'Plasmodium' named entity 'toxic' named entity 'histone deacetylase inhibitors' named entity 'potency' named entity 'antiplasmodial' named entity 'HDAC6' named entity 'HDAC inhibitors' named entity 'antiplasmodial' named entity 'future science group' named entity 'HDAC6' named entity 'CQS' named entity 'HDACs' named entity 'antiplasmodial' named entity 'dose-response curve' named entity 'toxicity' named entity 'pyrimethamine' named entity 'SIRT1' named entity 'mechanisms of action' named entity 'antiplasmodial' named entity 'homology' named entity 'dose-response curves' named entity 'antiplasmodial' named entity 'homology' named entity 'artemisinin combination therapies' named entity 'aromatic ring' named entity 'sulfadoxine' named entity 'class III' named entity 'artemisinin' named entity 'cytotoxicity' named entity 'parasite' named entity 'HDAC4' named entity 'ADME' named entity 'toxicity' named entity 'infection' named entity 'HDAC1' named entity 'antiplasmodial' named entity 'Chinese Hamster' named entity 'CQS' named entity 'parasite' named entity 'isoforms' named entity 'antiplasmodial' named entity 'indole' named entity 'inhibitory activity' named entity 'P. falciparum' named entity 'antiplasmodial' named entity 'therapeutic window' named entity 'genus' named entity 'malaria' named entity 'mode of action' named entity 'nanomolar' named entity 'antiplasmodial' named entity 'histone' named entity 'parasite' named entity 'HDAC6' named entity 'P. falciparum' named entity 'lactate dehydrogenase' named entity 'antiplasmodial' named entity 'P. falciparum' named entity 'Malaria' named entity 'hydroxamic acid' named entity 'parasite' named entity 'benzothiazepine' named entity 'P. falciparum' named entity 'infection'

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