Regulation of the Escherichia coli AtoSC two component system by synthetic biologically active 5;7;8-trimethyl-1;4-benzoxazine analogues

Filippou, Panagiota; Koini, Eftychia N.; Calogeropoulou, Theodora; Kalliakmani, Panagiota; Panagiotidis, Christos Α.; Kyriakidis, Dimitrios A.

doi:10.1016/j.bmc.2011.06.029

Cited by 10 publications

(2 citation statements)

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“…Compounds TC121, TC145 and TC158 were synthesized as previously reported. 30,31 The synthesis of compounds TC143, TC128, TC161 will be reported elsewhere.…”

Section: Methodsmentioning

confidence: 99%

Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Koukouli

Paspaltsis

Salta

et al. 2012

Prion

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Prion diseases are fatal, neurodegenerative diseases characterized by the structural conversion of the normal, cellular prion protein, PrP (C) into an abnormally structured, aggregated and partially protease-resistant isoform, termed PrP (Sc) . Although substantial research has been directed toward development of therapeutics targeting prions, there is still no curative treatment for the disease. Benzoxazines are bicyclic heterocyclic compounds possessing several pharmaceutically important properties, including neuroprotection and reactive oxygen species scavenging. In an effort to identify novel inhibitors of prion formation, several 5,7,8-trimethyl-1,4-benzoxazine derivatives were evaluated in vitro for their effectiveness on the expression levels of normal PrP (C) and its conversion to the abnormal isoforms of PrP (Sc) in a scrapie-infected cell culture model. The most potent compound was 2-(4-methoxyphenyl)-5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine, with a diminishing effect on the formation of PrP (Sc) , thus establishing a class of compounds with a promising therapeutic use against prion diseases.

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“…Compounds TC121, TC145 and TC158 were synthesized as previously reported. 30,31 The synthesis of compounds TC143, TC128, TC161 will be reported elsewhere.…”

Section: Methodsmentioning

confidence: 99%

Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Koukouli

Paspaltsis

Salta

et al. 2012

Prion

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“…Here we have chosen benzo[b] [1,4]oxazinyl class for the synthesis as these derivatives have a wide range of biological activities like, treatment of cardiovascular [5][6][7], antibacterial [8,9], antifungal [10][11][12], anticancer activity [13][14][15] and protein methyl transferases inhibitors [16]. Sulphonamide derivatives are considered as an important moiety in drug synthesis and have excellent antimicrobial activity [17].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antiproliferative evaluation of new (4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methane substituted sulfonamide derivatives

Pawar¹,

Sarkate²,

Karnik³

et al. 2017

Eur. J. Chem.

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Antimicrobial evaluation of 1,4-benzoxazine derivatives

et al. 2014

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Regulation of the Escherichia coli AtoSC two component system by synthetic biologically active 5;7;8-trimethyl-1;4-benzoxazine analogues

Cited by 10 publications

References 29 publications

Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Synthesis and antiproliferative evaluation of new (4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methane substituted sulfonamide derivatives

Antimicrobial evaluation of 1,4-benzoxazine derivatives

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Regulation of the Escherichia coli AtoSC two component system by synthetic biologically active 5;7;8-trimethyl-1;4-benzoxazine analogues

Cited by 10 publications

References 29 publications

Inhibition of PrPScformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Inhibition of PrPScformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Synthesis and antiproliferative evaluation of new (4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methane substituted sulfonamide derivatives

Antimicrobial evaluation of 1,4-benzoxazine derivatives

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Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives

Inhibition of PrP^Scformation in scrapie infected N2a cells by 5,7,8-trimethyl-3,4-dihydro-2H-1,4-benzoxazine derivatives