Bauer-7-en-3beta-yl acetate: a major constituent of unusual samples of Brazilian propolis

The pentacyclic triterpenoid bauer-7-en-3beta-yl acetate was obtained from the chloroform extract of an unusual sample of propolis from southeast Brazil with the yield of 7%. The compound was identified by comparison of IR, MS and NMR analysis with published data.

Antimycobacterial and cytotoxicity activities of free and liposome-encapsulated 3-(4'-bromo[1,1'-biphenyl-4-yl)-3-(4-bromo-phenyl)-N,N-dimethyl-2-propen-1-amine

The antimycobacterial activity of 3-(4'-bromo[1,1'-biphenyl-4-yl)-3-(4-bromo-phenyl)-N,N-dimethyl-2-propen-1-amine (BBAP), free or incorporated in preformed liposomes, on extracellular M. tuberculosis H37Rv was 8 and 25 μM (MIC), respectively. Extracellular antimycobacterial activity was not significantly improved by entrapment of BBAP in liposomes, but there was a 6.1-fold reduction of BBAP cytotoxicity on J774 macrophages. Liposomal BBAP or its free form showed IC50 values of 165 and 27 μM, resulting in a selectivity index (SI=IC50/MIC) of 3.4 and 6.6, respectively. Free BBAP in concentrations from 10 to 80 μM were quite effective in eliminating intracellular M. tuberculosis while liposomal formulation was less effective at these concentrations.

Synthesis and biological activity of n-{5-(4-methylphenyl) diazenyl-4-phenyl-1, 3-thiazol-2-yl}benzamide derivatives

In the present study, various amides of 2-amino-5-(4-methylphenyl)-diazenyl-4-phenyl-1, 3-thiazole was synthesized and their biological activities were evaluated. All the synthesized compounds were characterized by the combination of elemental analysis and standard spectroscopic methods. They are screened for anti-bacterial activity against Escherichia coli and Staphylococcus aureus as well as screened for antifungal activity against Aspergillus niger and Apergillus oryzae by cup plate method at 1 µg/ mL concentration in DMF.

Säätyläistutkimus Ylä-Savosta

Kirjallisuusarvostelu

Synthesis, characterization and computational studies of (E)-2-{[(2-aminopyridin-3-yl)imino]-methyl}-4,6-di-tert-butylphenol

(E)-2-{[(2-Aminopyridin-3-yl)imino]-methyl}-4,6-di-tert-butyl-phenol ( 3: ), a ligand containing an intramolecular hydrogen bond, was prepared according to a previous literature report, with modifications, and was characterized by UV-vis, FTIR, ¹H-NMR, 13C-NMR, HHCOSY, TOCSY and cyclic voltammetry. Computational analyses at the level of DFT and TD-DFT were performed to study its electronic and molecular structures. The results of these analyses elucidated the behaviors of the UV-vis and electrochemical data. Analysis of the transitions in the computed spectrum showed that the most important band is primarily composed of a HOMO→LUMO transition, designated as an intraligand (IL) charge transfer.

Analysis of the structural and electronic properties of 1-(5-Hydroxymethyl - 4 -[ 5 - (5-oxo-5-piperidin-1-yl-penta-1,3dienyl)-benzo[1,3]dioxol-2-yl] -tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4dione molecule

The structural and electronic properties of 1-(5-Hydroxymethyl - 4 -[ 5 - (5-oxo-5-piperidin- 1 -yl-penta- 1,3 -dienyl)-benzo [1,3] dioxol- 2 -yl]-tetrahydro -furan-2 -yl)-5-methy l-1Hpyrimidine-2,4dione (AHE) molecule have been investigated theoretically by performing density functional theory (DFT), and semi empirical molecular orbital calculations. The geometry of the molecule is optimized at the level of Austin Model 1 (AM1), and the electronic properties and relative energies of the molecules have been calculated by density functional theory in the ground state. The resultant dipole moment of the AHE molecule is about 2.6 and 2.3 Debyes by AM1 and DFT methods respectively, This property of AHE makes it an active molecule with its environment, that is AHE molecule may interacts with its environment strongly in solution.

Biheterocyclic ligands: synthesis, characterization and coordinating properties of bis(4-amino-5-mercapto-1,2,4-triazol-3-yl) alkanes with transition metal ions and their thermokinetic and biological studies

The Co(II), Ni(II) and Cu(II) metal ions complexes of Bis(4-amino-5-mercapto-1,2,4-triazol-3-yl) alkanes (BATs) have been prepared and characterized by elemental analysis, conductivity measurements infrared, magnetic susceptibility, the electronic spectral data and thermal studies. Based on spectral and magnetic results, the ligands are tetradentate coordinating through the N and S-atoms of BATs; six-coordinated octahedral or distorted octahedral and some times four-coordinated square planar were proposed for these complexes. Activation energies computed for the thermal decomposition steps were compared. The ligands and their metal complexes were tested in vitro for their biological effects. Their activities against two gram-positive, two gram-negative bacteria and two fungal species were found to vary from moderate to very strong.

Synthesis, spectroscopic characterization and antibacterial screening of novel n-(benzothiazol-2-yl)ethanamides

Synthesis, electronic, infrared, elemental micro analytical studies were carried on N-(benzothiazol-2-yl)trichloroethanamide [4] and N-(benzothiazol-2-yl)chloroethanamide [5]. They were also screened in vitro and in vivo for antibacterial activity. The results indicate that the compounds are very stable and that they show high antibacterial activities against both gram-positive and gram-negative bacteria tested. Both derivatives of 2-aminobenzothiazole were active against the multiresistant bacteria with IZD ranging from 9 -18 mm [5] and 9 - 20mm [4]. From the MIC results it is observed that the [5] derivative produced a better antibacterial activity than the [4] derivative. The lethal concentrations (LC50) of the compounds were also determined. Their solubilities and melting points were also determined.

Mikael Agricolan teosten kielen ala-, ylä-, ja -pää-vartaloiset adpositiot

Adpositions with the stems ala, ylä and pää in the language of Mikael Agricola’s writings The language of Mikael Agricola’s (c 1510–1557) writings represents an interesting phase in the development of the Finnish system for adpositions. In the Finnish language, the older Uralic system of postpositions has undergone expansion and a new system of prepositions has been adopted. On the other hand, the adposition system found in Agricola’s writings has also been strongly affected by foreign models, because Agricola’s texts are mainly translations of religious texts, which by and large use a word-for-word translation strategy. In the thesis, I explore Agricola’s use of adpositions; more specifically, which adpositions carry the meaning of ‘being under’ or ‘being over’ something, and in what other functions these adpositions are used. My main focus is on the semantics of the adpositions. I also study the syntactic features of adpositions and adposition structures; these are intertwined with semantics, since the meaning of adpositions is established in the adposition clause. Finally, I compare Agricola’s use of adpositions to the corresponding adpositions of present-day Finnish. Adpositions with stems ala, ylä and pää form an interesting subject for research. Their frequency in the data, however, is highly uneven. The overwhelming majority of the adpositions studied in the thesis are päälle; there are only two occurrences of adpositions with the stem ylä. Adpositions typically denote a location ‘under’ or ‘above’ something. Almost half of the adpositions, however, can be classified as semantically unmotivated and as representing a foreign model in terms of the Finnish language; they do not occur in present-day Finnish. In Agricola’s texts they act in more grammatical roles than the corresponding adpositions of present-day Finnish. In the thesis, the corresponding adpositions in the source languages are carefully analysed. All other uses of the adpositions are marginal in relation to spatial ones and those based on foreign models. The original meanings of the adpositions have not changed much since Agricola, but adpositions considered to originate from foreign models have been intentionally eliminated in presentday standard Finnish. It is also noteworthy that the system of adpositions with the stems ala, ylä and pää has changed since Agricola. His texts include the adposition ala, which corresponds to the modern adposition alle. Likewise the adposition yllä is absent in Agricola, as are the internal locative cases of the adposition pää.

Ylä-Savon liikenneturvallisuussuunnitelma : Sonkajärven liikenneturvallisuustyön toimintasuunnitelma

Ylä-Savon liikenneturvallisuussuunnitelma laadittiin seudun kuntien sekä Pohjois-Savon ELY-keskuksen yhteistyönä. Suunnitelmassa määriteltiin yhteiset seudulliset liikenneturvallisuuden ja esteettömyyden parantamista koskevat periaatteet. Seudullisten periaatteiden ja kuntakohtaisten erityispiirteiden ohjaamina laadittiin kunkin kunnan aikaisempien suunnitelmien päivitystarpeesta riippuen kuntakohtaiset liikenneympäristön parantamissuunnitelmat ja/tai liikenneturvallisuustyön toimintasuunnitelmat. Sonkajärvellä uusittiin liikenneturvallisuustyön toimintasuunnitelma. Liikenneturvallisuusongelmia kartoitettiin syksyn 2010 aikana tehdyillä liikenneilmapiiri ja -asennekyselyllä sekä vuosina 2005-2009 tapahtuneiden onnettomuuksien analyyseillä. Liikenneturvallisuusongelmien analysoinnin sekä valtakunnallisten ja Itä-Suomen liikenneturvallisuustavoitteiden pohjalta Ylä-Savon seudulle määritettiin yhteiset määrälliset ja toiminnalliset liikenneturvallisuustavoitteet. Määrälliseksi tavoitteeksi asetettiin, että kenenkään ei tarvitse kuolla tai loukkaantua vakavasti liikenteessä. Sonkajärven kunnan liikenneympäristön parantamistoimenpiteet on suunniteltu vuonna 2008 laaditussa liikenneympäristösuunnitelman päivitystyössä, minkä vuoksi tässä työssä ei suunniteltu uusia liikenneympäristön parantamistoimenpiteitä. Kokonaisvaltaisen liikenneturvallisuustyön toteutumisen seurannan helpottamiseksi aikaisemmin laaditut liikenneympäristön toimenpidekartat ja -taulukot kuitenkin päivitettiin ja liitettiin tähän suunnitelmaan. Hallintokuntakohtaiset liikenneturvallisuustyön toimintasuunnitelmat sisältävät liikenneturvallisuuskoulutuksen, -tiedotuksen ja -valistuksen toimenpiteet tuleville vuosille. Toimenpiteitä kohdistetaan kaikille ikäryhmille sisällyttäen liikenneturvallisuustyö kuntien palveluihin ja osaksi hallintokuntien jokapäiväistä työtä. Sonkajärvellä määritettiin myös kaikkien hallintokuntien yhteiset liikenneturvallisuustyön teemat tuleville vuosille. Vuonna 2012 teemana on ”Pyöräily ja muu kevyt liikenne”, vuonna 2013 ”Ikäihmiset liikenteessä”, vuonna 2014 ”Turvallinen liikenneympäristö” sekä vuonna 2015 ”Turvallisuutta liikenteeseen; oikealla asenteella ja nopeusrajoituksia noudattamalla”. Teeman valinnalla pyritään vaikuttamaan tärkeäksi koettuun kohderyhmään tai asiaan sekä tehostamaan hallintokuntien välistä yhteistyötä. Liikenneturvallisuussuunnitelman toteuttamista seurataan kunnan liikenneturvallisuustyöryhmässä, jonka kokoonpano tarkistettiin työn aikana. Ryhmään kuuluvat kunnan eri hallintokuntien edustajien lisäksi Liikenneturvan, poliisin ja Pohjois-Savon ELY-keskuksen edustajat.