Synthesis of new active nitrogen and sulfur containing norlabdanic compounds
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LUNGU, Lidia, BLAJA, Svetlana, CIOCARLAN, Alexandru, ILKER, Ozer, ARICU, Aculina, VORNICU, Nicoleta. Synthesis of new active nitrogen and sulfur containing norlabdanic compounds. In: Achievements and perspectives of modern chemistry, 9-11 octombrie 2019, Chişinău. Chisinau, Republic of Moldova: Tipografia Academiei de Ştiinţe a Moldovei, 2019, p. 226. 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

Synthesis of new active nitrogen and sulfur containing norlabdanic compounds


Pag. 226-226

Lungu Lidia1, Blaja Svetlana1, Ciocarlan Alexandru1, Ilker Ozer1, Aricu Aculina1, Vornicu Nicoleta2
 
1 Institute of Chemistry,
2 Metropolitan Center of Research TABOR, The Metropolitanate of Moldavia and Bukovina
 
 
Disponibil în IBN: 11 noiembrie 2019


Rezumat

The synthesis of hybrid terpeno-heterocyclic compounds is a recent concern of researchers in the field of natural products. Several papers describing the synthesis and biological activity of terpenic compounds bearing diazine [1,2], carbazole [2], triazole [2,3], oxadiazoleand thiadiazole [4] units have been recently published. It should be noted that the intermediates of terpenoheterocyclic compounds often exhibit biological activity. This communication confirms this fact and presents last-minute results. We report the synthesis of new di- and trinorlabdane thiosemicarbazides 1 and 2, tetranorlabdane 2-iminothiodiazole 3 and diacyl hydrazide 4, obtained in 60%-82% yields Figure 1. The structures of compounds 1-4 were fully confirmed by 1H, 13C and 2D NMR analysis.formulaFigure. New nitrogen and sulfur containing bioactive norlabdanes. Compounds 1-4 were tested in vitro for antifungal and antibacterial activity on five strains of fungi and both Gram-negative and Gram-pozitive bacteria (Table 1). Compound 3 have shown the best antifungal and antibacterial activity at (MIC) of 0.125 μg/mL and 2.5 μg/mL, respectively. Compounds 1, 2 and 4 possess activity comparable with reference compounds Caspofungin and Kanamycin (4 μg/mL). Table. Results of in vitro testing of antibacterial and antifungal activity of compounds 1-4.tabel

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<description xml:lang='en' descriptionType='Abstract'><p>The synthesis of hybrid terpeno-heterocyclic compounds is a recent concern of researchers in the field of natural products. Several papers describing the synthesis and biological activity of terpenic compounds bearing diazine [1,2], carbazole [2], triazole [2,3], oxadiazoleand thiadiazole [4] units have been recently published. It should be noted that the intermediates of terpenoheterocyclic compounds often exhibit biological activity. This communication confirms this fact and presents last-minute results. We report the synthesis of new di- and trinorlabdane thiosemicarbazides 1 and 2, tetranorlabdane 2-iminothiodiazole 3 and diacyl hydrazide 4, obtained in 60%-82% yields Figure 1. The structures of compounds 1-4 were fully confirmed by 1H, 13C and 2D NMR analysis.</p><p>formula</p><p>Figure. New nitrogen and sulfur containing bioactive norlabdanes. Compounds 1-4 were tested in vitro for antifungal and antibacterial activity on five strains of fungi and both Gram-negative and Gram-pozitive bacteria (Table 1). Compound 3 have shown the best antifungal and antibacterial activity at (MIC) of 0.125 &mu;g/mL and 2.5 &mu;g/mL, respectively. Compounds 1, 2 and 4 possess activity comparable with reference compounds Caspofungin and Kanamycin (4 &mu;g/mL). Table. Results of in vitro testing of antibacterial and antifungal activity of compounds 1-4.</p><p>tabel</p></description>
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