27 research outputs found

    Synthesis and Photochemical Behaviour of Substituted 3,4-furandicarboxdianilides

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    Same substituted 3,4-furandicarboxdianilides were prepared from the corresponding substituted anilines and 3,4-furandicarboxylic acid dichloride. All compounds were exposed to UV irradiation in methanolic solution, but under the conditions applied only p-chloro- substituted dianilide dehydrocyclized to the corresponding furo-bis-quinolone

    Photochemical Isomerizations of Furylacrylic Acids

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    It was shown that cis-3-(2\u27 -furyl)acrylic acid (lb), cis-2- methyl-3-(2\u27 -furyl)acrylic acid (Ilb), cis-3-(5\u27 -methyl-2\u27 -furyl) acrylic acid (IIIb) and cis-2-methyl-3-(5\u27-methyl-2\u27 -furyl)acrylic acid (!Vb) can be conveniently prepared by photochemical isomerization of the corresponding trans acids (Ia-IVa). The rate of isomerization and the composition of the mixture at photoequi- 1ibrium in water-filtered ultraviolet is not influenced by methyl substitution. The isomeric acids were separated through their cyclohexylammonium salts and characterized by elemental analyses, uv. and ir. spectra

    Photochemical Isomerizations of Furylacrylic Acids

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    It was shown that cis-3-(2\u27 -furyl)acrylic acid (lb), cis-2- methyl-3-(2\u27 -furyl)acrylic acid (Ilb), cis-3-(5\u27 -methyl-2\u27 -furyl) acrylic acid (IIIb) and cis-2-methyl-3-(5\u27-methyl-2\u27 -furyl)acrylic acid (!Vb) can be conveniently prepared by photochemical isomerization of the corresponding trans acids (Ia-IVa). The rate of isomerization and the composition of the mixture at photoequi- 1ibrium in water-filtered ultraviolet is not influenced by methyl substitution. The isomeric acids were separated through their cyclohexylammonium salts and characterized by elemental analyses, uv. and ir. spectra

    Osvrt na održani znanstveno-stručni skup "Vladimir Prelog i hrvatska kemija"

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    Synthesis and Biological Activity of Substituted Benzothiazole Derivatives

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    U posljednjih nekoliko desetljeća postoji velik interes za razvoj malih heterocikličkih molekula kao potencijalnih terapeutika. U tu skupinu spada i velik broj derivata benzotiazola, koji pokazuju zanimljiva kemijska i bioloÅ”ka svojstva, te se u posljednjih nekoliko desetljeća znatno povećalo zanimanje za pripravu različitih derivata benzotiazola i njihovo bioloÅ”ko ispitivanje. U ovom članku opisane su neke od metoda dobivanja benzotiazolnih derivata te je dan pregled nekih od derivata benzotiazola s bioloÅ”kim djelovanjem.Despite improvements in survival rates, cancer and viral diseases remain the second leading cause of death in the western world. Therefore, an area of major pharmaceutical interest over the last several decades has been the development of small molecules with antitumor and antiviral activity. Two potential targets for compounds with antitumor and antiviral activity are DNA and different types of proteins like tyrosine kinases or topoisomerase I/II. Therefore, the design of new intercalators, groove-binders and discovery of specific inhibitors of proteins are two important approaches in the search for new chemotherapeutic agents. Over the past decade, development of small heterocyclic molecules as potential therapeutics has been an area of major interest. A large number of benzothiazole derivatives are of considerable biological and chemical interest. In the last several decades there has been a significant increase in the preparation of benzothiazole derivatives and their biological activity. Many 2-substituted benzothiazoles have been reported to display a large panel of biochemical properties, including antibacterial, antitumor, antiviral and antibiotic activities. Variation of substituents on the benzothiazole nuclei could potentially affect the interaction of the molecules with biological targets. Benzothiazole compounds received much attention from medicinal as well as synthetic organic chemists, not just due to their potential as biologically active compounds, but also as tools to study and visualize DNA. Because of their capacity to penetrate through cell membranes they were proposed for DNA visualization in fluorescent microscopy. These types of compounds are also interesting because of their applications in several areas as materials in electronics, as optical polymers and as anticorrosive protection

    Synthesis and Biological Activity of Substituted Benzothiazole Derivatives

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    U posljednjih nekoliko desetljeća postoji velik interes za razvoj malih heterocikličkih molekula kao potencijalnih terapeutika. U tu skupinu spada i velik broj derivata benzotiazola, koji pokazuju zanimljiva kemijska i bioloÅ”ka svojstva, te se u posljednjih nekoliko desetljeća znatno povećalo zanimanje za pripravu različitih derivata benzotiazola i njihovo bioloÅ”ko ispitivanje. U ovom članku opisane su neke od metoda dobivanja benzotiazolnih derivata te je dan pregled nekih od derivata benzotiazola s bioloÅ”kim djelovanjem.Despite improvements in survival rates, cancer and viral diseases remain the second leading cause of death in the western world. Therefore, an area of major pharmaceutical interest over the last several decades has been the development of small molecules with antitumor and antiviral activity. Two potential targets for compounds with antitumor and antiviral activity are DNA and different types of proteins like tyrosine kinases or topoisomerase I/II. Therefore, the design of new intercalators, groove-binders and discovery of specific inhibitors of proteins are two important approaches in the search for new chemotherapeutic agents. Over the past decade, development of small heterocyclic molecules as potential therapeutics has been an area of major interest. A large number of benzothiazole derivatives are of considerable biological and chemical interest. In the last several decades there has been a significant increase in the preparation of benzothiazole derivatives and their biological activity. Many 2-substituted benzothiazoles have been reported to display a large panel of biochemical properties, including antibacterial, antitumor, antiviral and antibiotic activities. Variation of substituents on the benzothiazole nuclei could potentially affect the interaction of the molecules with biological targets. Benzothiazole compounds received much attention from medicinal as well as synthetic organic chemists, not just due to their potential as biologically active compounds, but also as tools to study and visualize DNA. Because of their capacity to penetrate through cell membranes they were proposed for DNA visualization in fluorescent microscopy. These types of compounds are also interesting because of their applications in several areas as materials in electronics, as optical polymers and as anticorrosive protection

    Stereoisomeric 2-Naphthyl-3-furylacrylic Acids. Synthesis, Separation and Identification

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    Some new 2-(a-naphthyl)- and 2-(~-naphthyl)-3-furylacrylic acids were synthetized by modified Perkin reaction. The separable mixture of stereoisomeric acids were obtained in each case. The identity of Z and E isomers were assigned on the basis of NMR data

    Cyclic Benzimidazole Derivatives and Their Antitumor Activity

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    U posljednjih nekoliko godina interes za proučavanem kemije benzimidazola znatno je porastao zbog njihovog Å”irokog spektra bioloÅ”kog djelovanja, kao i mnogobrojnih mogućnosti primjene kao materijala u elektronici, u elektrokemiji za zaÅ”titu od korozije, polimera ili optičkih materijala. Struktura benzimidazola sadržana je u vitaminu B12 kao i u strukturi mnogih terapeutskih agensa koji imaju antitumorsko, antiinfektivno, antibakterijsko, antifungalno i mnoga druga bioloÅ”ka djelovanja. Ciklički derivati benzimidazola poput benzimidazo[1,2-a]kinolina, benzimidazo[1,2- -c]kinazolina, benzimidazo[2,1-b]izokinolina kao i mnogi drugi privukli su znatnu pažnju kako organskih sintetskih tako i medicinskih kemičara zbog interesantnih bioloÅ”kih značajki, ponajprije vrlo dobrog antitumorskog djelovanja. Ciklički derivati benzimidazola imaju planarnu strukturu koja im omogućuje interkaliranje između parova baza dvostruke uzvojnice DNA. Interkalativni način vezivanja danas je jedan od najvažnijih u djelovanju antitumorskih lijekova.Over the past years benzimidazole derivatives are one of the most extensively studied classes of heterocyclic compounds, and have received much attention from synthetic organic as well as medicinal chemists, because of their well known biological activities and their applications in several areas as materials in electronics, in electrochemistry as anticorrosive agents, as polymers or optical materials and fluorescent tags in DNA sequencing. The structure of vitamin B12, as an example, contains a benzimidazole group. Compounds containing benzimidazole nuclei show anticancer, antineoplastic, antiinfective, antibacterial, antifungal and many others activities. Due to the structural similarity of benzimidazole nuclei with some naturally occurring compounds such as purine, they can easily interact with biomolecules of the living systems. The introduction of an additional substituent on the benzimidazole nuclei has been increasing attention in the expectation that such changes could potentially affect the interaction of the molecules with biological targets. Fused cyclic benzimidazole derivatives, as benzimidazo[1,2-a]quinolines,benzimidazo[1,2-c]quinazolines, benzimidazo[2,1-b]isoquinolines and many others, have also interesting biological activities and most of them are very good anticancer agents. DNA is the molecular target of many anticancer drugs in clinical use and development. Compounds which can bind to DNA with intercalative or non-intercalative mechanism play a major role in biological processes such as gene transcription or DNA replication. Benzoannulated benzimidazole analogues contain a planar chromophore and have the ability to become inserted between adjacent base pairs of DNA double helix. Intercalators are recognized as one of the most important classes of anticancer agents. So an understanding of the drug-DNA interactions is a promising approach to developing novel reagents and plays a key role in pharmacology today
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