About: Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis

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About: Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis Goto Sponge NotDistinct Permalink

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

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis
Creator	Kumar, Vipan Hall, Dominique Hopper, Melissa Patel, Neal Raj, Raghu Sharma, Vaishali Wrischnik, Lisa Hall, Á Hopper, M Kirkwood, • Kumar, Á Land, M Land, Á Patel, Á Raj, R Sharma, Á Wrischnik, L
Source	PMC
abstract	In this study, we describe the synthesis of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates using copper-catalysed azide-alkyne cycloaddition reaction between mono- and di-propargylated azetidin-2-ones and N-alkylazido isatins. The synthesized conjugates were evaluated for their preliminary in vitro analysis against Trichomonas vaginalis at 50 μM. The efficacy of synthesized hybrids was observed to depend on the substituent at N-1 position of β-lactam ring, as well as the presence of single/double 1H-1,2,3-triazole linker. Among the synthesized conjugates, the presence of a p-tolyl substituent at N-1 of β-lactam ring was preferred for good activity profiles while the increase in spacer length did not influence the efficacy of the compounds. Compounds with high levels of potency were further analysed to determine their IC(50) values, as well as cytotoxicity profiles against mammalian cells. The most active compound in the synthesized conjugates displayed an IC(50) value of 10.49 μM against cultured G3 strain of T. vaginalis and was non-toxic to cultured mammalian HeLa cells at the same concentration. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1007/s00044-014-0956-6) contains supplementary material, which is available to authorized users.
has issue date	2014-02-22(xsd:dateTime)
bibo:doi	10.1007/s00044-014-0956-6
has license	no-cc
sha1sum (hex)	24af4ebcbb6c2d6478f93dcca107655daaea72f9
schema:url	https://doi.org/10.1007/s00044-014-0956-6
resource representing a document's title	Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis
has PubMed Central identifier	PMC7080013
schema:publication	Med Chem Res
resource representing a document's body	covid:24af4ebcbb6c2d6478f93dcca107655daaea72f9#body_text
is schema:about of	named entity 'cells' named entity 'ring' named entity 'compound' named entity 'IN VITRO' named entity 'USING' named entity 'COPPER' named entity 'THEIR' named entity 'ACTIVE' named entity 'CONCENTRATION' named entity 'CYCLOADDITION REACTION' named entity 'GOOD' named entity 'MAMMALIAN' named entity 'LACTAM RING' named entity 'LACTAM' named entity 'ALKYNE' named entity 'VALUES' named entity 'OBSERVED' named entity 'COMPOUND' named entity 'MONO' named entity 'INFLUENCE' named entity 'LINKER' named entity 'TRICHOMONAS VAGINALIS' named entity 'LENGTH' named entity 'CELLS' named entity 'VALUE' named entity 'PATHOGEN' named entity 'SYNTHESIS' named entity 'LEVELS' named entity 'HUMAN' named entity 'NON-' named entity 'TOXIC' named entity 'VAGINALIS' named entity 'AZIDE' named entity 'DESCRIBE' named entity 'POTENCY' named entity 'HYBRIDS' named entity 'DEPEND' named entity 'EFFICACY' named entity 'INCREASE' named entity 'EVALUATED' named entity 'PREFERRED' named entity 'TRIAZOLE' named entity 'CULTURED' named entity 'STUDY' named entity 'HELA CELLS' named entity 'DETERMINE' named entity 'ISATIN' named entity 'SPACER' named entity 'STRAIN' named entity 'TETHERED' named entity 'ABSTRACT' named entity 'ANALYSIS' named entity 'CONJUGATES' named entity 'CYTOTOXICITY' named entity 'DID' named entity 'IN VITRO ACTIVITY' named entity 'PROTOZOAL' named entity 'PRELIMINARY' named entity 'HIGH' named entity 'BIS' named entity 'POSITION' named entity 'PRESENCE OF' named entity 'DISPLAYED' named entity 'SUBSTITUENT' named entity 'SINGLE' named entity 'ACTIVITY' covid:arg/24af4ebcbb6c2d6478f93dcca107655daaea72f9

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