2-(2-Nitro­anilino)-4,5,6,7-tetra­hydro­benzo[b]thio­phene-3-carbonitrile

The title compound, C15H13N3O2S, was synthesized by the reaction of 2-amino-5,6,7,8-tetra­hydro-4H-cyclo­hepta­[b]thio­phene-3-carbonitrile and o-fluoro­nitro­benzene. The dihedral angle between the thio­phene and nitro­phenyl rings is 75.15 (2)°. In the crystal, inter­molecular N—H⋯N and C—H⋯O inter­actions lead to the formation of a supra­molecular chain extending along the c-axis direction

2-Amino-4,5,6,7-tetra­hydro­benzo[b]thio­phene-3-carbonitrile

The title compound, C9H10N2S, was synthesized according to Gewald procedures by the reaction of cyclo­hexa­none with malonitrile and sulfur in the presence morpholine. The cyclo­hexane ring adopts a half-chair conformation and the thio­phene ring is essentially planar (r.m.s. deviation = 0.05 Å). The crystal packing is stabilized by two inter­molecular N—H⋯N hydrogen bonds, which link the mol­ecules into centrosymmetric rings with graph-set motif R 2 2(12)

Preliminarno ispitivanje antimikotskog i citotoksičnog djelovanja derivata cikloalkil[b]tiofena PLS-DA analizom

A series of 2-[(arylidene)amino]-cycloalkyl[b]thiophene-3-carbonitriles (2a-x) was synthesized by incorporation of substituted aromatic aldehydes in Gewald adducts (1a-c). The title compounds were screened for their antifungal activity against Candida krusei and Criptococcusneoformans and for their antiproliferative activity against a panel of 3 human cancer cell lines (HT29, NCI H-292 and HEP). Forantiproliferative activity, the partial least squares (PLS) methodology was applied. Some of the prepared compounds exhibited promising antifungal and proliferative properties. The most active compounds for antifungal activity were cyclohexyl[b]thiophene derivatives, and forantiproliferative activity cycloheptyl[b]thiophene derivatives, especially 2-[(1H-indol-2-yl-methylidene)amino]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carbonitrile (2r), which inhibited more than 97 % growth of the three cell lines. The PLS discriminant analysis (PLS-DA)applied generated good exploratory and predictive results and showed that the descriptors having shape characteristics were strongly correlated with the biological data.Koristeći supstituirane aromatske aldehide u Gewaldovim aduktima 1a-c sintetizirani su derivati 2-[(ariliden)amino]-cikloalkil[b]tiofen-3-karbonitrila (2a-x). Ispitano je antimikotsko djelovanje tih spojeva na gljivice Candida krusei i Criptococcus neoformans te antiproliferativno djelovanje na tri humane tumorske stanične linije (HT29, NCI H-292 i HEP). Za antiproliferativno djelovanje primijenjena je metoda parcijalnih najmanjih kvadrata (PLS) koristeći softverski program Pentacle. Neki od ispitanih spojeva pokazuju obećavajuće antimikotsko i antiproliferativno djelovanje. Najjače antimikotsko djelovanje imaju cikloheksil[b]tiofen derivati, a najjače antiproliferativno djelovanje cikloheptil[b]tiofen derivati, posebice 2-[(1H-indol-2-il-metiliden)amino]-5,6,7,8-tetrahidro-4H-ciklohepta[b]tiofen-3-karbonitril (2r), koji inhibira više od 97 % rast svih triju ispitivanih staničnih linija. Primijenjena PLS diskriminirajuća analiza dala je dobre istraživačke i prognostičke rezultate i pokazala da deskriptori dobro koreliraju s biološkim rezultatima

1,4‐Dithiane‐2,5‐diol: An Attractive Platform for the Synthesis of Sulfur Containing Functionalized Heterocycles

This microreview highlights the utility of 1,4? dithiane?2,5?diol 1 as a source for the in situ generation of 2?mercaptoacetaldehyde 2, a versatile two?carbon synthon featuring both electrophilic and nucleophilic reaction centers widely utilized as an attractive platform for the preparation of sulfur?containing molecules. We discussed the involved chemistry, mainly focusing on its applications to the construction of sulfur?containing heterocyclic compounds including the thiophene and 1,3?thiazole families and other different sulfur?nitrogen and sulfur?oxygen heterocycles which continue to be a pillar of organic synthesis as a result of their broad application in organic and medicinal chemistry

Attitudes of teachers in kindergartens to physical activity

The aim of this work is to look into the issue of kindergarten teachers and theircompetency in the area of physical education. These competencies reflect the teachers' personal attitudes derived from the quality of their lives, their wellbeing. The attitudes of kindergarten teachers towards physical education were surveyed by a questionnaire method (Wear's standardized questionnaire) and then evaluated and interpreted. Thorough analysis of these data is preceded by basic theoretic definition of the term "quality of life" and attitudes from the area of psychology and kinanthropology. Other widely used methods of gathering attitudes are also briefly mentioned

Reaction of Substituted Furan-2-carboxaldehydes and Furo[b]pyrrole Type Aldehydes with Hippuric Acid

4-Heteroarylidene-2-phenyl-1,3-oxazol-5(4H)-ones were prepared by reactions of hippuric acid with substituted furan-2-carboxaldehydes or furo[b]pyrrole type aldehydes. The reactivity of various furan-2-carboxaldehyde derivatives in this reaction is discussed. The effect of microwave irradiation on some condensation reactions was compared with “classical” conditions. The results show that microwave irradiation shortens the reaction times while affording comparable yields. Elementary analysis, UV, IR and 1D NMR proved the structure of new synthesised compounds. 2D NMR spectroscopic measurements confirmed that the configuration at the carbon-carbon double bond corresponds to the pure E isomers of the products

Reactions of Substituted Furan-2-carboxaldehydes and Furo[b]pyrrole Type Aldehydes with Benzothiazolium Salts

A series of new push-pull compounds were synthesised by reaction of 5-aryl- furan-2-carboxaldehydes and furo[b]pyrrole type aldehydes with benzothiazolium salts. These new condensation products represent highly conjugated systems that have potential biological activity. The reaction of furo[b]pyrrole type aldehydes with benzothiazolium salts give potential precursors of cyanine dyes

Eucaryotic Genomes Comparison

Hlavním motivem pro vznik této diplomové práce byla potřeba kvalitních bioinformatických nástrojů, které slouží na porovnávání genomů a vylepšení jednoho z existujících nástrojů - RepeatExplorer. Práce přináší přehled transposibilních elementů v DNA, existujících nástrojů určených pro identifikaci a analýzu repetic v nasekvenovaných genomech. V práci jsou popsány nedostatky nástroje RepeatExplorer se zaměřením na komparativní analýzu genomů. Byly navrženy a implementovány dvě řešení k odstranění těchto nedostatků. První řešení je určeno na porovnávání dvojic genomů. Princip tohoto řešení je založen na porovnávání podobnosti rozložení pokrytí contigů prostřednictvím Kolmogorov-Smirnova testu, díky čemu víme určiť rozdílné místa v genomech. Druhé řešení, které slouží k porovnávání více genomů, je založeno na metodě mapování readů porovnávaných genomů na contigy referenčního genomu a poskytuje grafy s pokrytím contigů, pomocí kterých víme určit variabilitu repetic. Funkčnost byla ověřena na reálných NGS datech organizmu Silene latifolia.Main motive of this master thesis was the need of good bioinformatics tools for genome comparison and improvement of one of the existing tools - RepeatExplorer. This work offers an overview of transposable elements in DNA, existing tools for identification and analysis of repetitions in sequenced genomes, summary of currently used genome sequencing methods. This work describes shortcomings of RepeatExplorer tool with focus on comparative analysis of genomes. Two solutions to remove these problems were designed and implemented. The first solution is designed for comparing pairs of genomes. The principle of this solution is based on comparison of similarity of distribution of contigs coverages using Kolmogorov-Smirnov test, thanks to which we are able to determine different parts in the genomes.The second solution, which is used to compare multiple genomes, is based on the method of mapping reads from compared genomes to the reference genome contigs and provides contigs coverage graphs, by which we are able to determine the variability of the repeats.Their functionality was verified on real NGS data of organism Silene latifolia.