Acilpiruvati kao prekursori u sintezi nekih biološki aktivnih jedinjenja

Rezime: U ovoj disertaciji sintetisana je serija acilpiruvata u visokim prinosima reakcijom Klajzenove kondenzacije. Acilpiruvati su zatim korišćeni kao prekursori za sintezu tri nove klase jedinjenja pod pretpostavkom da će pokazati bolja biološka svojstva od samih acilpiruvata. Sintetisana je serija od dvadeset i pet novih 1,5- diaril-4-(2-tienilkarbonil)-3-hidroksi-3-pirolin-2-oni. Pored toga, bilo je veoma interesantno ispitati kako koordinacija za neke jone prelaznih metala utiče na aktivnost organskih molekula kao što su acilpiruvati. Zbog toga je sintetisano jedanaest novih metalo-organskih kompleksa sa acilpiruvatima kao ligandima koji sadrže Cu2+ ili Pd2+ kao centralni jon metala. Sva novo-sintetisana jedinjenja su okarakterisana spektroskopskom analizom (UV-Vis, IR, 1H i 13C NMR), masenom spektrometrijom i elementalnom analizom. Rendgenska strukturna analiza je takođe urađena gde je to bilo moguće. Novosintetizovani molekuli testirani su na antioksidativni, antimikrobni i antitumorski potencijal. DPPH test pirolidinona je pokazao da ova jedinjenja poseduju dobru antioksidativnu aktivnost (najniža IC50 vrednost iznosi 166,75 µg/ml). Ovaj test je takođe pokazao da većina acilpiruvata poseduje bolju antioksidativnu aktivnost od odgovarajućih metalo-organskih jedinjenja bakra(II). Ispitivanja antimikrobne aktivnosti su otkrila da pirolidinoni pokazuju značajnu inhibitorsku aktivnost na soju bakterija Staphylococcus aureus u prilično niskim koncentracijama (najniža izmerena MIC vrednost iznosi 0,312 mg/ml), dok je najosetljiviji soj gljivica bio Trichophyton mentagrophytes sa najnižom MIC od 0,625 mg/ml. MIC vrednosti za metalo-organska jedinjenje bakra(II) na testiranim mikroorganizmima bile su u rasponu od 0,048 do 3,125 mg/ml. Najosetljiviji soj bakterija bio je Proteus mirabilis, dok je među gljivicama najosetljiviji soj bio Candida albicans.SUMMARY: In this dissertation a series of acylpyruvates in high yields has been synthesized using the Claisen condensation reaction, which were then used as precursors for the synthesis of three new classes of compounds. Three new classes of compounds were synthesized under the assumption that they would show better biological properties than the acylpyruvates themselves. A series of twenty-five novel and one previously published 1,5-diaryl-4-(2-thienylcarbonyl)-3-hydroxy-3- pyrrolin-2-ones were synthesized. In addition, it was very interesting to examine how coordination for some metal ion affects the activity of organic molecules such as acylpyruvates, and therefore eleven new metal-organic complexes were synthesized with acylpyruvates as ligands containing Cu2+ or Pd2+ as the central metal ion. All newly synthesized compounds were characterized by spectroscopic analysis (UV-Vis, IR, 1H and 13C NMR), mass spectrometry and elemental analysis. X-ray structural analysis was also performed where possible. The newly synthesized molecules were tested for antioxidant, antimicrobial and antitumor potential. The DPPH test showed that most acylpyruvates showed better antioxidant activity than the corresponding metal-organic copper(II) compounds. MIC values for the metalorganic copper(II) compounds on the tested microorganisms were in range from 0.048 to 3.125 mg/ml. The most sensitive bacteria strain was Proteus mirabilis, while among the fungi the most sensitive strain was Candida albicans. The results of the antitumor activity showed that these compounds showed good cytotoxic activity. All metal-organic copper(II) compounds showed lower IC50 values on the LS174 and A549 cell lines compared to cisplatin. The results of the antitumor potential for palladium(II) metal-organic complexes showed that the three compounds had very good cytotoxic activity on HeLa cells and significant activity on MDA-MB 231 cells. The results obtained by examining the interations between the palladium compound and cisplatin indicate that these compounds may be useful as adjuvants in therapy for the treatment of tumors, reducing the doses of cisplatin and thus the side effects of this drug

Development of the transmission tower virtual 3D model for structural analysis in ANSYS

U ovom radu je opisana metodologija 3D modeliranja stuba dalekovoda. Zadatak je bio da se razvije virtualni 3D model, u potpunosti odgovarajući realnoj strukturi, koji će biti podvrgnut strukturalnoj analizi u ANSYS programskom paketu. Proces 3D modeliranja je od suštinskog značaja za ovaj postupak kompijuterske analize. Metoda zahteva precizno definisanje koordinata čvornih tačaka. I to ne samo ključnih čvornih tačaka strukture, nego i tačaka koje će biti važne za buduću analizu napona i deformacija. Ovo znači da osoba koja radi na kreiranju modela treba da bude dobro upoznata sa metodom strukturne analize kako bi unapred predodredila sve tačke koje su od značaja za konstrukciju i za analizu. Težište eksperimenta je određivanje dinamičkog ponašanja strukture izložene poznatom opterećenju. 3D model koji je u korelaciji sa stvarnom konstukcijom, sa potvrđenom geometrijom, statičkim i dinamičkim karakteristikama pruža priliku da se predvidi ponašanje strukture pod opterećenjima koja ne mogu da se primene na stvarne konstrukcije (ekstremna preopterećenja, kompleksna opterećenja i oštri vremenski uslovi).This paper describes a methodology for transmission tower 3D modelling. The task was to develop a virtual 3D model, corresponding to the real structure, which will be subjected to structural analysis in ANSYS software. The process of 3D modelling is crucial for this kind of computer analysis. It requires precise key point coordinates defining. Not only the important points of the structure, but also the points of interest for the future structural analysis have to be defined. This means that model developer should be familiar with the structural analysis so he could form adequate key points in advance. The main point of the experiment concept is to determine dynamic behaviour of the structure, exposed to a known load. Truly correlated 3D model, with verified geometric, static and dynamic properties offers the opportunity to predict the structure behaviour under loads that can hardly apply on a living structure (extreme overloads, complex loads, and harsh ambient condition)

Effect of time of desiccation on oil content in different sunflower hybrids

Chemical desiccation with Reglone Forte has been tried in production fields under four sunflower hybrids. Reglone Forte (2 l/ha) was applied at 7-day intervals from the end of pollination till maturity. Seed moisture was determined prior to each treatment. Seed oil content was determined at maturity, using the method of nuclear magnetic resonance. The highest oil content was found in the control, the lowest in the treatment 7 days after flower (DAF). The absence of significant differences among treatments 21 DAF, 28 DAF and the control was an indication that there was no large increment in oil content in the period after the average seed moisture reached 44.34% and maturity. Considering individual hybrids, there was no large oil content increase already from treatment 14 DAF, with the exception of hybrid NS-H-43 which evidently required a later treatment. Considering the time of treatment in relation to seed moisture, this hybrid achieved maximum oil content when treated at 31% seed moisture. In hybrid NS-H-26 RM, however, maximum oil content was achieved with treatment at 25% seed moisture

Fenotipska i genotipska varijabilnost dužine krunice cevastog cveta i sadržaja nektara kod suncokreta

The nectar content and disc flower corolla length are the two most important parameters of attractiveness to pollinators in sunflower. The phenotypic and genotypic variability of these two traits was studied in four commercially important hybrids and their parental components in a trial with three fertilizer doses over two years. The results showed that, looking at individual genotypes, the variability of disc flower corolla length was affected the most by year (85.38-97.46%). As the study years were extremely different, the phenotypic variance of the hybrids and parental components was calculated for each year separately. In such conditions, looking at all of the crossing combinations, the largest contribution to phenotypic variance of the corolla length was that of genotype: 57.27-61.11% (NS-H-45) 64.51-84.84% (Velja); 96.74-97.20% (NS-H-702) and 13.92-73.17% (NS-H-111). A similar situation was observed for the phenotypic variability of nectar content, where genotype also had the largest influence, namely 39.77-48.25% in NS-H-45; 39.06-42.51% in Velja; 31.97-72.36% in NS-H-702; and 62.13-94.96% in NS-H-111.Najznačajniji parametri atraktivnosti za oprašivače kod suncokreta su sadržaj nektara i dužina krunice cevastog cveta. Fenotipska i genotipska varijabilnost ovih svojstava je izučavana kod 4 komercijalno važna hibrida i njihove roditeljske komponente u ogledu sa 3 doze đubrenja, u dve godine. Rezultati istraživanja pokazuju da je na varijabilnost dužine krunice cevastog cveta bio najznačajniji uticaj godine (85.38-97.46%), ako se ona posmatra za pojedinačne genotipove. Pošto su godine istraživanja bile ekstremno različite fenotipska varijansa je izračunata za hibride i roditeljske komponente za svaku godinu posebno. U takvim okolnostima za sve kombinacije ukrštanja najveći udeo u fenotipskoj varijansi za dužinu krunice cevastog cveta je imao genotip: 57.27-61.11% (NS-H-45); 64.5l-84.84% (Velja); 96.74-97.20% (NS-H-702) i 13.92-73.17% (NS-H-111). Slično je bilo i sa fenotipskom varijabilnošću za sadržaj nektara, jer je takodje bio najznačajniji uticaj genotipa i to: 39.77-48.25% kod NS-H-45; 39.06-42.51% kod Velja; 31.97-72.36% kod NS-H-702162.13-94.96% kod NS-H-111

Način nasleđivanja i heritabilnost dužine krunice cevastog cveta i sadržaja nektara kod suncokreta

Since disc flower corolla length and nectar content are the two most important parameters of attractiveness to pollinators in sunflower and we monitored them in the parental lines F[ hybrids, we thought it would be interesting to determine the mode of inheritance and heritability of these two traits. The mean values of disc flower corolla length ranged between 7.23-10.22 mm. Differences among most of the genotypes were significant Year had significant influence on the expression of this trait. In the inheritance of the corolla length, partial dominance of the parent with the smaller corolla length (NS-H-702) was observed when determining mode of inheritance relative to the parents. Relative to the parental average however it was not possible to determine the mode of inheritance in any of tile hybrid combinations. The nectar content means ranged from 2.08 to 15.54 mg/20 flowers and differences among most of the genotypes were significant. Partial dominance of the parent with the smaller nectar content mean was recorded in the inheritance of this trait (NS-H-702): Negative heterosis was found in the hybrid NS-H-45.Pošto su dužina krunice cevastog cveta i sadržaj nektara najvažniji parametri atraktivnosti genotipova suncokreta za oprašivače i praćeni su kod roditeljskih linija i F1 hibrida bilo je interesantno utvrditi način nasleđivanja i heritabilnost za ova dva svojstva. Srednje vrednosti za dužinu krunice cevastog cveta su se kretale od 7.23-10.22mm. Razlike su bile značajne između većine ispitivanih genotipova. Na ekspresiju dužine krunice cevastog cveta su značajno uticale godine. U nasleđivanju ovoga svojstva ispoljila se parcijalna dominacija roditelja sa manjom dužinom krunice cevastog cveta (NS-H-702) i to u slučaju utvrđivanja načina nasleđivanja u odnosu na roditelje, dok u odnosu na roditeljski prosek nije bilo moguće utvrditi način nasleđivanja ni u jednoj hibridnoj kombinaciji. Srednje vrednosti za sadržaj nektara su se kretale od 2.08-15.54mg/20 cvetova i razlike su bile značajne kod većine ispitivanih genotipova. U nasleđivanju sadržaja nektara se ispoljila parcijalna dominacija roditelja sa manjom srednjom vrednošću za ovo svojstvo (NS-H-702), dok se kod hibrida NS-H-45 ispoljio negativni heterozis

Međuzavisnost uslova oprašivanja, oplodnje i prinosa semena suncokreta

Four commercially important sunflower hybrids (NS-H-45, NS-H-l 11, NS-H-702 and Velja) and their parental components (Ha-74B, Ha-98B, CMS-3-8B, Ha-26B, RHA-583, RHA-R-PI-2/1 and RHA-113N) were used over a period of two years to study the following traits: disk flower corolla length, nectar content, pollen viability, bee visitation, fertilization percentage and seed yield. Relations among the traits were determined by path coefficient analysis. The simple correlation coefficients showed that fertilization percentage and bee visitation had a highly significant influence on seed yield. The corolla length had a positive effect on nectar content, while nectar content had a significant negative influence on pollen viability. The highest significant direct influence on seed yield was that of fertilization percentage, while the effect on nectar content on seed yield was negative but not significant. The coefficient of determination was 0.8071.Kod četiri komercijalno važna hibrida suncokreta (NS-H-45, NS-H-111, NS-H-702 i Velja) i njihovih roditeljskih komponenti (Ha-74B, Ha-98B, CMS-3-8B, Ha-26B, RHA-583, RHA-R-P1-2/1 i RHA-113N) u dve godine su ispitivana sledeća svojstva: dužina krunice cevastog cveta, sadržaj nektara, vitalnost polena, poseta pčela, % oplodnje i prinos semena. Međuzavisnost ispitivanih svojstava je utvrđena Path coefficient analizom. Prosti koeficijenti korelacije su pokazali da su % oplodnje i poseta oprašivača imali visoko značajan pozitivan uticaj na prinos semena. Značajan pozitivan efekat je imala dužina krunice na sadržaj nektara, a značajan negativan efekat je imao sadržaj nektara na vitalnost polena. Najveći značajan direktan efekat na prinos semena je imao procenat oplodnje, dok je negativan, ali ne i značajan efekat imao sadržaj nektara na prinos semena. Koeficijent determinacije je iznosio 0,8071

Limitirajući faktori u proizvodnji semenskog suncokreta u 1999. godini

The production of seed sunflower, like any other seed production, has its own peculiarities and additional requirements that often do not appear in commercial production. First of all, one must be much more rigorous when-choosing the plot and the crop rotation must be adhered to without exception. Also, the herbicides and their doses must be decided upon carefully and the plots must be kept free of weeds all the way through until harvesting. Certain additional requirements may present themselves when carrying out the other crop tending measures as well. Of course, there is also the problem of spatial isolation to prevent contamination by unwanted pollen. Still, the largest differences between the two types of production are related to sunflower pollination. .Proizvodnja semenskog suncokreta kao i svaka semenska proizvodnja odlikuje se odgovarajućim specifičnostima i dodatnim zahtevima koji se često ne javljaju u merkantilnoj proizvodnji. Kao prvo mora se biti rigorozniji pri izboru parcele i striktno poštovati plodored. Mora se voditi računa pri izboru herbicida kao i njihovih doza a parcele se moraju održavati čistim od korova sve do žetve. Određeni dodatni zahtevi mogu se javiti i prilikom izvođenja drugih mera nege. Naravno, tu je i problem prostorne izolacije radi sprečavanja kontaminacije nepoželjnim polenom. Ipak najveće razlike vezane su za oplodnju suncokreta

Pojam hibridnog rata

nem

Osnovni principi proizvodnje hibridnog semena suncokreta

Sunflower seed production has certain attributes that make it different of ordinary sunflower production and seed production of other crops. This is, at first, isolation and pollination with fertilization. In our country isolation determined by low is 3 km for parental line production, and 2 km for hybrid seed sunflower production. Sometimes it is not enough, since some of the pollinators could fly much longer distances. Pollinators' attractivety of some sunflower genotypes differ, but influence of environmental factors to pollination and fertilization is bigger.Proizvodnja semena suncokreta se odlikuje odgovarajućim specifičnostima koje je razlikuju u odnosu na proizvodnju merkantilnog useva, kao i na proizvodnju semenskih useva drugih kultura. Kod suncokreta se to pre svega odnosi na specifičnosti vezane za prostornu izolaciju, kao i oprašivanje i oplodnju. U našoj zemlji propisana je prostorna izolacija od 3 km za proizvodnju baznog odnosno 2 km za proizvodnju hibridnog semena suncokreta što ponekad nije dovoljno, jer pojedini polinatori lete mnogo dalje. Atraktivnost pojedinih genotipova ka polinatorima se razlikuje ali veći uticaj na oprašivanje i oplodnju imaju spoljašnji činioci

Implementation of inverted classroom methodology in 3D modeling course

3D modeliranje u SolidWorks-u se predaje na Mašinskom fakultetu Univerziteta u Beogradu (Srbija) više od jedne decenije. Kao i svaka nova veština koju treba savladati, softverski paket SolidWorks zahteva dobro prilagođenu metodologiju podučavanja. Najbolji mogući način podučavanja bio bi individualni mentorski rad. Jedan profesor po studentu, koji bi bio apsolutno fokusiran na završetak zadatka studenta, i pružio najbolje rezultate . Nažalost, zbog nedostatka nastavnog osoblja i velikog broja studenata, ovaj pristup nije moguć. Umesto toga, jedan profesor bi predstavio zadatak iz 3D modeliranja grupi od 80 studenata. Oni bi pratili celokupnu prezentaciju i tek kada se završi celokupna prezentacija, studenti bi se podelili u četiri učionice sa po 20 računara i vežbali predstavljene zadatke. Tokom poslednje decenije primećeno je nekoliko velikih problema u ovim nastavnim metodama. Primenjen je novi pristup nastavi. Ovaj rad predstavlja novu metodologiju nastave i postignute rezultate u poboljšanju nastavnog procesa.More than one decade 3D modeling in SolidWorks is taught at the Faculty of Mechanical Engineering at the University of Belgrade (Serbia). As every new skill that has to be mastered, SolidWorks software package demands well-tailored teaching methodology. The best possible way of teaching would be one-on-one tutoring. One teacher per student, who would be absolutely focused on student's task completion, would provide the best results. Unfortunately, due to the lack of teaching staff and vast number of students this approach isn't possible. Instead, one teacher would present the 3D modeling task of interest on the video presenter to a group of 80 students. They would follow the whole presentation and only when the whole presentation ends, students would split into four classrooms with 20 computers each, and practice the presented tasks. During the last decade few major problems in these teaching methods were recognized. A new teaching approach was implemented. This paper presents a novel teaching methodology and achieved results in the teaching process improvement