Tetrahydroisoquinoline alkaloids are a class of structurally complex natural products and a huge number of its natural product widely exist in nature which, from the discovery has been more than a century, it compounds with high anti-tumor activity, antibacterial and other physical activity, but also because of its special structure, with low oncentration of biological activity, but these alkaloids are not sold in the market mainly due to a less natural extraction, chemical synthesis method and multi-step, low yield. Therefore, we constructed a combination of tetrahydroisoquinoline alkaloids and the pyrazino [2,1-b] quinazoline-3,6-diones structure of the new compounds, which have the quinazolinone compounds which is the drug synthesis and drug activity on the bond, is also a kind of unique and widely used drug structure, and causes a lot of scientists and drug research interest and discussion, as we develop the motivation.

A systematic study was carried out for the synthesis of aziridine 2-phosphonates by using two methods. First method is the classical Gabriel-Cromwell reaction and the second one is the modified version of Gabriel-Cromwell reaction which was developed in this thesis. In the first method, vinyl phosphonate was used as the starting material, then it was brominated to get 1,2-dibromoethyl phosphonate. HBr elimination from this compound, then reaction with different primary amines gave desired aziridinyl phosphonates in good yields. In the second method, easily available acetyl phosphonate was used as the starting material which was reacted with DBU and tosyl chloride to get &alpha / -tosylated vinyl phosphonate. Reaction of this compound with the same amines gave aziridinyl phosphonates in good yields, as well. Biological activities of all newly synthesized compounds were studied against different bacteria.

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Darbo tikslas: atlikti preparatų, turinčių augalinių žaliavų kaupiančių rozmarino rūgštį, sudėčių palyginamąją analizę, nustatyti bendrą fenolinių junginių kiekį, rozmarino rūgšties kiekį ir antioksidacinį aktyvumą. Darbo uždaviniai:  Išrinkti preparatus su rozmarino rūgštimi;  Atlikti šių preparatų sudėčių palyginamąją analizę;  Nustatyti ir palyginti bendrą fenolinių junginių kiekį preparatuose;  Nustatyti ir palyginti rozmarino rūgšties kiekį ESC metodu;  Nustatyti ir palyginti antioksidacinį aktyvumą. Tyrimo objektai ir metodai: preparatai, turintys augalines žaliavas, kaupiančias rozmarino rūgštį ir kvapiųjų rozmarinų skystasis ekstraktas. Bendras fenolinių junginių kiekio nustatymas atliktas spektrofotometriniu būdu, naudojant standartinį Folin – Ciocalteu reagentą. Rozmarino rūgšties kiekis preparatuose nustatytas ESC metodu. Antioksidacinis aktyvumas nustatytas DPPH radikalo sujungimo metodu. Literatūros analizės metodu atlikta rozmarino rūgšties preparatų sudėčių analizė. Išvados: Tyrimams išrinkti 3 kompleksiniai preparatai su kvapiųjų rozmarinų augaline žaliava ir skystasis rozmarinų ekstraktas. Daugiausia kvapiųjų rozmarinų žaliavos ir RR kiekio RPD buvo keturkomponentiniame Verdin. Žaliavos dalis sudaro 50,68 % preparato. Atlikus bendro fenolinių junginių kiekio tyrimą, nustatyta, kad didžiausias fenolinių junginių kiekis yra skystajame rozmarinų ekstrakte (160,34 RRE mg/ml) (P<0.05). Didžiausias rozmarino rūgšties kiekis rastas skystajame rozmarinų... [toliau žr. visą tekstą] / Aim: to make comparable analysis of preparations containing plant materials accumulating rosmarinic acid, determine the total phenolic compound content, rosmarinic acid content and compare antioxidant activity. Objective:  Elect the preparations with rosmarinic acid;  Make the comparative analysis of compositions of these preparations;  Determine and compare the total phenolic compound content;  Determine and compare the rosmarinic acid content using HPLC method;  Determine and compare their antioxidant activity. Objects and methods: products with plant materials accumulating rosmarinic acid and rosemary leaf liquid extract. Total content of phenolic compounds was carried out spectrophotometrically using a standart Folin- Ciocalteu reagent. Rosmarinic acid content was determined by HPLC method. Antioxidant activity determined by DPPH radical scavenging method. The comparable analysis of products composition performed by literary analysis method. Conclusion: For research were selected 3 complex preparations with rosemary plant material and liquid rosemary extract. The highest quantity of raw rosemary material and RR quantity in RDD had Verdin, the preparation containing 4 components. Rosemary plant material makes 50,68 % in the preparation. Total phenolic compounds study showed that the highest amount of phenolic coumpounds had liquid rosemary extract (160,34 RAE mg/ml). The biggest quantity of rosmarinic acid was found in liquid rosemary extract (0.03 mg/ml). Combined... [to full text]

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.

Neovibsanin A and B are natural products which induced neurite outgrowth in PC12 cells. They belong in the neovibsane class under the rare vibsane natural product family, whose structures are characterized by polycyclic, polyoxygenated cores. Based on a proposed biosynthesis, the synthetic strategy towards neovibsanin A and B involved synthesizing a key enone intermediate. Initial investigation using this intermediate lead to the total synthesis of 2-O-methylneovibsanin H. Crucial to this concise synthesis was an acid-catalyzed, one-pot, four-step cascade reaction. Modifying the reaction condition leads to a different five-step cascade pathway, resulting in the total synthesis of 4,5-bis-epi-neovibsanin A and B. The synthetic trials and tribulations encountered on the road to these final compounds are explored. It is envisaged that other related neovibsane natural products may arise based on this synthetic sequence. 4,5-Bis-epi-neovibsanin A and B, as well as several other structural analogues collected during the synthesis, were biologically assayed using NGF-stimulated PC12 cells. All compounds induced a significant proportion of neurons to extend neurite processes compared to control cultures. The structure-activity relationship studies indicated that the tricyclic core, as well as the 3,3-dimethylacroyl enol ester side chain, may be responsible for promoting a biological response.