Browsing by Subject "Thiazoles"
Now showing items 1-11 of 11
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Article
In silico exploration for identifying structure-activity relationship of MEK inhibition and oral bioavailability for isothiazole derivatives
(2010)In this study, quantitative structure-activity/property models are developed for modeling and predicting both MEK inhibitory activity and oral bioavailability of novel isothiazole-4-carboxamidines. The models developed are ...
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Article
Inactivation of the glutamine/amino acid transporter ASCT2 by 1,2,3-dithiazoles: Proteoliposomes as a tool to gain insights in the molecular mechanism of action and of antitumor activity
(2012)The ASCT2 transport system catalyses a sodium-dependent antiport of glutamine and other neutral amino acids which is involved in amino acid metabolism. A library of 1,2,3-dithiazoles was designed, synthesized and evaluated ...
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Doctoral Thesis Open Access
New chemistry of 1,2,3-dithiazoles
(Πανεπιστήμιο Κύπρου, Σχολή Θετικών και Εφαρμοσμένων Επιστημών / University of Cyprus, Faculty of Pure and Applied Sciences, 2012-01)Το ενδιαφέρον μας στη χημεία των 1,2,3-διθειαζολών προκύπτει από το γεγονός ότι τα διθειαζολικά συστήματα μπορούν να χρησιμοποιηθούν στην προετοιμασία νέων ετεροκυκλικών συστημάτων με σημαντικές βιολογικές ιδιότητες. Ένας ...
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Article
New regiospecific isothiazole C-C coupling chemistry
(2006)Regioselective palladium catalysed coupling reactions are achieved in good to high yields, starting from either 3,5-dichloro- or 3,5-dibromoisothiazole-4-carbonitriles 1 and 2, providing 3-halo-5-(hetero/aryl, alkenyl and ...
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Doctoral Thesis Open Access
New ring transformations of 1,2,3-dithiazoles
(Πανεπιστήμιο Κύπρου, Σχολή Θετικών και Εφαρμοσμένων Επιστημών / University of Cyprus, Faculty of Pure and Applied Sciences, 2017-01)Ο αρχικός στόχος της παρούσας Διατριβής ήταν η διερεύνηση της αντίδρασης μετασχηματισμού Ν-αζινυλ-1,2,3-διθειαζολιμινών προς αζινο-θειαζόλες. Μελέτη της αντίδρασης αυτής οδήγησε στην ανάπτυξη μιας νέας και αποδοτικής ...
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Article
One-step conversion of 2-Amino- N ′-arylbenzamidines into 3-aryl-4-imino-3,4-dihydroquinazoline-2-carbonitriles using 4,5-dichloro-1,2,3- dithiazolium chloride
(2013)2-Amino-N′-arylbenzamidines react with 4,5-dichloro-1,2,3- dithiazolium chloride (Appel salt) in the presence of Hünig's base (2 equiv) to give in one step 3-aryl-4-imino-3,4-dihydroquinazoline-2-carbonitriles in 53-81% ...
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Article
A qualitative comparison of the reactivities of 3,4,4,5-Tetrachloro-4H-1,2,6-thiadiazine and 4,5-Dichloro-1,2,3-dithiazolium Chloride
(2015)The high yielding transformations of 3,4,4,5-tetrachloro-4H-1,2,6-thiadiazine into 3,5-dichloro-4H-1,2,6-thiadiazin-4-one (up to 85%) and 2-(3,5-dichloro-4H-1,2,6- thiadiazin-4-ylidene)malononitrile (up to 83%) have been ...
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Article
The reaction of 4,5-Dichloro-1,2,3-dithiazolium chloride with sulfimides: A new synthesis of N-Aryl-1,2,3-dithiazolimines
(2009)N-Aryl-S,S-dimethylsulfimides 3 (Ar = 4-NO2C6H4), 4 (Ar = Ph) and 5 (Ar = 4- Tol) react with Appel salt 1 to give the corresponding N-aryl-(4-chloro-5H-1, 2,3- dithiazolylidene)benzenamines 8 (Ar = 4-NO2C6H4), 9 (Ar = Ph) ...
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Article
Reinvestigating the reaction of 1H-pyrazol-5-amines with 4,5-dichloro-1,2,3-dithiazolium chloride: A route to pyrazolo[3,4-c]isothiazoles and pyrazolo[3,4-d]thiazoles
(2014)The reaction of Appel salt 1 with 1H-pyrazol-5-amines 2 gives main products N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-1H-pyrazol-5-amines 3, and 6H-pyrazolo[3,4-c]isothiazole-3-carbonitriles 5, together with several minor ...
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Article
Silver-mediated palladium-catalyzed direct C-H arylation of 3-bromoisothiazole-4-carbonitrile
(2011)Silver(I) fluoride-mediated Pd-catalyzed C-H direct arylation/ heteroarylation of 3-bromoisothiazole-4-carbonitrile (1a) gives twenty-four 5-aryl/heteroaryl-3-bromoisothiazole-4-carbonitriles. The reaction was partially ...
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Article
Synthesis of [(4-Chloro-5H-1,2,3-dithiazol-5-ylidene)amino]azines
(2011)The reactions of 2-, 3- and 4-aminopyridines with 4,5-dichloro-1,2,3- dithiazolium chloride (Appel salt) 4 to give N-(4-chloro-5H-1,2,3-dithiazol-5- ylidene)pyridin-Xamines 1a (X = 2), 1g (X = 3) and 1k (X = 4) were optimized ...