cas 5558-95-2, 2-(TRICHLOROMETHYL)QUINAZOLIN-4(3H)-ONE | Articles data ｜lookchem

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5558-95-2

Articles about 5558-95-2Total 4 be found

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Sonogashira cross-coupling reaction in 4-chloro-2- trichloromethylquinazoline series is possible despite a side dimerization reaction
We studied the Sonogashira coupling reaction between 4-chloro-2- trichloromethylquinazoline and various terminal alkynes, mainly in phenylacetylene series. A brief review of the literature shows that mono- or polybromo/chloromethylated substrates, especia
Kieffer, Charline,Verhaeghe, Pierre,Primas, Nicolas,Castera-Ducros, Caroline,Gellis, Armand,Rosas, Roselyne,Rault, Sylvain,Rathelot, Pascal,Vanelle, Patrice
p. 2987 - 2995
(2013/03/29)

Targeting the human malaria parasite Plasmodium falciparum: In vitro identification of a new antiplasmodial hit in 4-phenoxy-2- trichloromethylquinazoline series
From the promising results we previously obtained in quinazoline series and to complete the evaluation of the in vitro antiplasmodial activity of original 2-trichloromethylquinazolines, we synthesized new quinazolines possessing a variously substituted phenoxy group at position 4 through a simple and efficient two-step-synthesis approach. The studies of their activity toward the multi-resistant W2 Plasmodium falciparum strain and of their cytotoxicity on the human hepatocyte HepG2 cell line highlighted a hit compound (molecule 7) displaying a W2 IC50 value of 1.1 μM and a HepG2 CC50 value of 50 μM, comparable to chloroquine and doxycycline. Structure-activity- and toxicity relationships indicate that the trichloromethyl group plays a key role in the antiplasmodial activity of such chemical scaffold and also that the phenoxy group substitution as a direct influence on the molecules selectivity. Moreover, molecule 7 displays significant specific activity against the Plasmodium genus in comparison with Toxoplasma and does not show any mutagenic property at the Ames test.
Castera-Ducros, Caroline,Azas, Nadine,Verhaeghe, Pierre,Hutter, Sebastien,Garrigue, Philippe,Dumtre, Aurelien,Mbatchi, Litaty,Laget, Michle,Remusat, Vincent,Sifredi, France,Rault, Sylvain,Rathelot, Pascal,Vanelle, Patrice
experimental part
p. 4184 - 4191
(2011/11/29)

QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY
The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.
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Page/Page column 16-17

(2008/12/08)

SIMPLE METHOD FOR THE SYNTHESIS OF 2-TRICHLOROMETHYL-4-QUINAZOLONES
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Vovk, M. V.,Samarai, L. I.
p. 559
(2007/10/02)

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Chemical Properties

Melting Point: 211-213°C(lit.)
Boiling Point: 330.8 °C at 760 mmHg
Flash Point:153.9 °C
Density: 1.64g/cm³
Vapor Pressure: 0.000162mmHg at 25°C
Refractive Index: 1.673
PSA: 45.75000
LogP: 2.74980

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