About: Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones

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About: Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones Goto Sponge NotDistinct Permalink

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

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones
Creator	Balzarini, Jan Orzeszko, Andrzej Orzeszko-Krzesińska, Barbara Maurin, Jan
source	Elsevier; Medline; PMC
abstract	Abstract A series of novel thiazolidin-4-ones bearing a lipophilic adamantyl substituent at position 2 or 3 were synthesized. A majority of them showed a modest anti-HIV-1 activity, whereas 2-adamantan-1-yl-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (8) was endowed with a remarkable antiviral potency (EC50 =0.67μM). The new series of compounds (22–29) with an adamantyl moiety at the 3-position of the thiazolidinone ring showed good to modest anti-HIV-1 activity (EC50 =1.0–11μM) but also pronounced cytostatic activity. For example 24, 26 and 29 showed an EC50 of 1.0–2.0μM, while the 50% effective concentrations for 23 and 28 were 7.8 and 11.0μM, respectively. X-ray studies and quantum chemical calculations revealed that the anti-HIV activity of the compounds strongly depends on their dipole moments and conformation of the thiazolidinones.
has issue date	2009-01-31(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2008.02.039
bibo:pmid	18420310
has license	els-covid
sha1sum (hex)	4dc98948c7e50a6d03b16a4cfb35a54553b773ce
schema:url	https://doi.org/10.1016/j.ejmech.2008.02.039
resource representing a document's title	Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones
has PubMed Central identifier	PMC7127420
has PubMed identifier	18420310
schema:publication	European Journal of Medicinal Chemistry
resource representing a document's body	covid:4dc98948c7e50a6d03b16a4cfb35a54553b773ce#body_text
is schema:about of	named entity 'ring' named entity 'studies' named entity 'Synthesis' named entity 'STUDIES' named entity 'THEIR' named entity 'GOOD' named entity 'CYTOSTATIC' named entity 'MOIETY' named entity 'EXAMPLE' named entity 'ANTI-HIV ACTIVITY' named entity 'SYNTHESIZED' named entity '2C6' named entity '0.67' named entity 'MODEST' named entity 'CHEMICAL' named entity 'EFFECTIVE' named entity 'BEARING' named entity 'QUANTUM' named entity 'ACTIVITY' named entity 'POSITION' named entity 'NEW' named entity 'RING' named entity 'BUT' named entity 'DIPOLE MOMENTS' named entity 'THIAZOLIDINONE' named entity 'X-RAY' named entity 'CONFORMATION' named entity 'LIPOPHILIC' named entity 'STUDIES' named entity 'ANTI-HIV-1 ACTIVITY' named entity 'NOVEL' named entity '288' named entity 'REVEALED' named entity '50%' named entity 'ANTI-HIV' named entity 'MAJORITY' named entity 'SUBSTITUENT' named entity 'ANTIVIRAL' named entity 'POTENCY' named entity 'SERIES' named entity 'SYNTHESIS' named entity 'ADAMANTAN' named entity 'CONCENTRATIONS' covid:arg/4dc98948c7e50a6d03b16a4cfb35a54553b773ce named entity 'activity' named entity 'series' named entity 'calculations' named entity 'antiviral' named entity 'anti-HIV' named entity 'conformation' named entity 'substituent' named entity 'anti-HIV' named entity 'basis set' named entity 'chlorine' named entity 'France' named entity 'eluent' named entity '4.3' named entity 'adamantyl' named entity 'adamantane' named entity 'dipole moments' named entity 'effective concentration' named entity 'DNA and RNA' named entity 'antiviral' named entity 'anti-HIV' named entity 'antiviral activity' named entity 'THF' named entity 'potential density' named entity 'nitrogen atom' named entity 'heterocycle' named entity 'ethyl' named entity 'adamantyl' named entity 'methyl' named entity 'HIV-2' named entity 'isomer' named entity '35 mM' named entity 'cell cultures' named entity 'HIV-1' named entity 'cell cultures'

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