About: Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties

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About: Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties Goto Sponge NotDistinct Permalink

An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.benthamdirect.org/pages/b_viewarticle.php?articleID=3176129
Description	A set of 2-benzylsulfanyl derivatives of benzothiazole was synthesized and evaluated for antimicrobial and cytotoxic activities. The biological screening on antimicrobial activity against a panel of Gram-positive and Gram-negative bacteria, yeasts and fungi identified benzylsulfanyl derivatives of benzothiazole as selective inhibitors of mycobacteria. The lead compounds in the set, dinitro derivatives exhibited significant activity against sensitive and multidrug-resistant strains of M. tuberculosis and low cytotoxicity. The QSAR study indicated that the antituberculotic activity is connected with LUMO and HOMO energies. The lower lipophilicity and the increased size of the molecule contribute to antituberculotic activity. Thus, dinitrobenzylsulfanyl derivatives of benzothiazole represent promising small-molecule synthetic antimycobacterials. A set of 2-benzylsulfanyl derivatives of benzothiazole was synthesized and evaluated for antimicrobial and cytotoxic activities. The biological screening on antimicrobial activity against a panel of Gram-positive and Gram-negative bacteria, yeasts and fungi identified benzylsulfanyl derivatives of benzothiazole as selective inhibitors of mycobacteria. The lead compounds in the set, dinitro derivatives exhibited significant activity against sensitive and multidrug-resistant strains of M. tuberculosis and low cytotoxicity. The QSAR study indicated that the antituberculotic activity is connected with LUMO and HOMO energies. The lower lipophilicity and the increased size of the molecule contribute to antituberculotic activity. Thus, dinitrobenzylsulfanyl derivatives of benzothiazole represent promising small-molecule synthetic antimycobacterials. (en)
Title	Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties (en)
skos:prefLabel	Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties Structure-Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties (en)
skos:notation	RIV/00216208:11160/12:10124337!RIV13-MZ0-11160___
http://linked.open...avai/riv/aktivita	I P Z
http://linked.open...avai/riv/aktivity	I, P(NS10367), Z(MSM0021620822)
http://linked.open...iv/cisloPeriodika	2
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Klimešová, Věra Palát, Karel Kočí, Jan
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Karlova v Praze / Farmaceutická fakulta v Hradci Králové
http://linked.open...dnocenehoVysledku	171907
http://linked.open...ai/riv/idVysledku	RIV/00216208:11160/12:10124337
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	cytotoxicity; antimicrobial activity; multidrug-resistant M. tuberculosis; Mycobacterium tuberculosis; Benzothiazole (en)
http://linked.open.../riv/klicoveSlovo	antimicrobial activity cytotoxicity Mycobacterium tuberculosis Benzothiazole multidrug-resistant M. tuberculosis
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[0C451D196B20]
http://linked.open...i/riv/nazevZdroje	Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	Evaluation and development of new perspective antimycobacterial drugs and prodrugs active against multidrug resistant strains
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	8
http://linked.open...iv/tvurceVysledku	Kočí, Jan Palát, Karel Stolaříková, Jiřina Klimešová, Věra Dahse, Hans-Martin Moellmann, Ute
http://linked.open...ain/vavai/riv/wos	000302993200017
http://linked.open...n/vavai/riv/zamer	Research of new drug structures
issn	1573-4064
number of pages	12 (xsd:int)
http://localhost/t...ganizacniJednotka	11160

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