Facultatea de Chimie şi Tehnologie Chimică / Faculty of Chemistry and Chemical Technology

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    SUBSTITUTED 1,3-PHENYL(PYRIDYL) PROPENONES AND DERIVATIVES WITH THIOSEMICARBAZIDIC GROUPS. STRUCTRURE – (HL-60) ANTILEUKEMIA ACTIVITY RELATIONSHIP
    (2014) Popușoi, Ana; Barba, Nicanor; Gulea, Aurelian; Roy, Jenny; Poirier, Donald
    3-(4-(Dimethylamino)phenyl-1-(4-isothiocyanatophenyl)prop-2-en-1-one was obtained from the corresponding N,N-dimethylthyoureas by elimination of dimethylamine at heating with gaseous hydrogen chloride in chloroform and 1-(4-isothiocyanatophenyl)-3-(pyridin-2-il)prop-2-en-1-one by treating 1,1-dimethyl-3-(4-(3-(pyridin-2-il)-acryloyl)-phenyl)thyourea with acetic anhydride. For all obtained compounds in the course of reaction the antileukemia activity was investigated.
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    SYNTHESIS AND BIOLOGIC PROPERTIES OF SOME1-(ALCHYL) PHENYL-3-(4-(3-(PYRIDIN-2-IL)ACRYLOYL)PHENYLTHIOUREA
    (2013) Popușoi, Ana; Barba, Nicanor; Gulea, Aurelian; Roy, Jenny; Poirier, Donald; Prisacari, Viorel
    This paper describe the synthesis of some 1-(alchyl)aril-3-(4-(3-pyridin-2-il) acryloyl)phenylthiourea obtained by condensation of 2-pyridincarboxaldehide with some derivatives of 4-acetylphenilthioureas in basic medium or by addition of aliphatic and aromatic amines to the correspondingisothiocyanatopropenones. 12 new compounds were obtained and their biological properties were analysed. The substituted thioureas by pyridine radicals, morpholine and phenol show a maximum bacteriostatic activity for Gram positive microorganisms like: Staphylococcus Aureus and Enterococcus Faecalis at the minimum inhibitory concentration 9.37-37.5 μM. Antifungal activity for Candida Albicans, Aspergillus Niger, AspergillusFumigatus, Penicillium is weak, in minimum inhibitory concentration 600->600 μM. The leukemia activity like inhibitor (HL-60), is 84-96.9% at the concentration 10-5mol/l and 15-20% and at the concentrations 10-6, 10-7mol/l.
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    SUBSTITUTED 1,3-PHENYL(PYRIDYL) PROPENONES AND DERIVATIVES WITH THIOSEMICARBAZIDIC GROUPS. STRUCTRURE – (HL-60) ANTILEUKEMIA ACTIVITY RELATIONSHI
    (Institute of Chemistry of ASM, 2014) Popuşoi, Ana; Barba, Nicanor; Gulea, Aurelian; Roy, Jenny; Poirier, Donald
    3-(4-(Dimethylamino)phenyl-1-(4-isothiocyanatophenyl)prop-2-en-1-one was obtained from the corresponding N,N-dimethylthyoureas by elimination of dimethylamine at heating with gaseous hydrogen chloride in chloroform and 1-(4-isothiocyanatophenyl)-3-(pyridin-2-il)prop-2-en-1-one by treating 1,1-dimethyl-3-(4-(3-(pyridin-2-il)-acryloyl)-phenyl)thyourea with acetic anhydride. The difference in the reactivity of the groups >C=O and NCS in the synthesis with hydrazine hydrate and its derivatives allows the synthesis of some 1,3-disubstituted propenones with thiosemicarbazide groups (4- and 1,4-disubstituted) in good yields. From 4-substituted thiosemicarbazides and 2-formilpyridine thiosemicarbazones were obtained. In the case of some derivatives, the propenone group in the reaction with hydrazine hydrate allows the formation of pyrazole derivatives. All obtained compounds were investigated for antileukemia activity. It was found that this activity is more pronounced for thiosemicarbazide derivatives with two pyridine nuclei at concentrations 10-5-10-7 mol/L.