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SM ISO690:2012 GUŢU, Iacob, SADOHIN, Vladimir, CALANCEA, Sergiu, BUȘILĂ, Maria, PRISACARU, Viorel. Synthesis and biologic properties of some N'-((3-aryl-1-phenyl-1hpyrazol-4-yl)methylene) isonicotinohydrazides. In: Achievements and perspectives of modern chemistry, 9-11 octombrie 2019, Chişinău. Chisinau, Republic of Moldova: Tipografia Academiei de Ştiinţe a Moldovei, 2019, p. 55. ISBN 978-9975-62-428-2. |
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Achievements and perspectives of modern chemistry 2019 | ||||||
Conferința "International Conference "Achievements and perspectives of modern chemistry"" Chişinău, Moldova, 9-11 octombrie 2019 | ||||||
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Pag. 55-55 | ||||||
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Pyrazole derivatives have found vigorous use as components of new bioactive substances, especially in the composition of some drugs. The pronounced biological activity of several pyrazole derivatives has spurred research into obtaining new compounds with additional heterocyclic structures. Of particular interest are pyrazole-4-carbaldehydes, which have a higher reactivity carbonyl group. In the present work as a condensing agent with isonicotinic acid hydrazide (isoniazid) - an effective medicine for the treatment of active tuberculosis, was proposed these aldehydes.3-Aryl-1-phenyl-1H-pyrazole-4-carbaldehydes were synthesized by the Vilsmeier-Haack reaction, from the ring substituted phenylhydrazones of the acetophenones and the Vilsmeier reagent. The synthesis method of pyrazolecarbaldehydes has been modified by using phosphorus pentachloride as a reagent for obtaining the Vilsmeier reagent. The 3-aryl-1-phenyl-1H-pyrazole4-carbaldehydes obtained were condensed with isonicotinic acid hydrazide. The structure of obtained N'-((3-aryl-1-phenyl-1H-pyrazol-4-yl) methylene)- isonicotinohydrazides 1 was confirmed based on IR spectra, 1H-NMR and 13C-NMR. Isonicotinohydrazides 1 were subjected to a virtual screening through the PASS (Prediction of Activity Spectra for Substation) program, the results of which showed that synthesized isonicotinohydrazines would exhibit antituberculous, antiviral and antimicrobial activity. The antibacterial activity (bacteriostatic and bactericidal) under laboratory conditions of the substances 1 was investigated for the microorganisms: Staphylococcus aureus, Staphylococcus epidermidis, Enteroccocus faecalis, Escherihia coli, Pseudomonas aeruginosa, Acinetobacter baumannii. The investigation results show that the 4-chloro derivative posses bacteriostatic activity for Gram-positive microorganism Staphylococcus Aureus at concentration of 75 μg/mL. Bacteriostatic and bactericidal action of substances 1 is at concentrations above 300 micro M for all test bacterial cultures investigated. |
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