New Multi-1,2,3-Selenadiazole Aromatic Derivatives

Al-Smadi, Mousa; Ratrout, Samer

doi:10.3390/10091126

Cited by 10 publications

(2 citation statements)

References 20 publications

(18 reference statements)

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“…A total of twelve synthesized multi-arm benzene derivatives of 1,2,3-selenadiazole and 1,2,3-thiadiazole by M. Al-Smadi et al [33,34,35] were selected for the present study. The in vitro inhibitory activity of the compounds against the human Glo-I enzyme was measured using double-beam UV-Vis spectrophotometer (Biotech Engineering Management Co. Ltd., UK).…”

Section: Methodsmentioning

confidence: 99%

Multi-Armed 1,2,3-Selenadiazole and 1,2,3-Thiadiazole Benzene Derivatives as Novel Glyoxalase-I Inhibitors

et al. 2019

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Glyoxalase-I (Glo-I) enzyme was established to be a valid target for anticancer drug design. It performs the essential detoxification step of harmful byproducts, especially methylglyoxal. A robust computer-aided drug design approach was used to design and validate a series of compounds with selenium or sulfur based heterorings. A series of in-house multi-armed 1,2,3-selenadiazole and 1,2,3-thiadiazole benzene derivatives were tested for their Glo-I inhibitory activity. Results showed that these compounds bind Glo-I active sites competitively with strong potential to inhibit this enzyme with IC50 values in micro-molar concentration. Docking poses revealed that these compounds interact with the zinc atom at the bottom of the active site, which plays an essential role in its viability.

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Section: Methodsmentioning

confidence: 99%

Multi-Armed 1,2,3-Selenadiazole and 1,2,3-Thiadiazole Benzene Derivatives as Novel Glyoxalase-I Inhibitors

et al. 2019

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“…Acidification of the mixture by adding a few drops of acetic acid gave a precipitate which was recrystallised from ethanol to get compounds (2 a-c ). (18) .…”

Section: General Procedures For the Preparation Of 23-bis (4-methoxypmentioning

confidence: 99%

Cyclization of Semicarbazones to 1,2,3-Selenadiazoles By Selenium Dioxide

Al-Obaidy¹

2012

J.Edu.Sci.

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In the present work some of 1,2,3-selenadiazole compounds derived from corresponding semicabazones have been prepared. The reaction of substituted chalcone compounds (1a-c) and 4-methoxy benzyl cyanide give compounds (2a-c) which were converted through the reaction with semicarbazide hydrochloride into the corresponding semicarbazones (3a-d(. The treatment of these compounds with selenium dioxide leads to ring closure of semicarbazones to give the 1,2,3-selenadiazole compounds. The structures of the synthesized compounds were established by physical and spectral methods.

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