Sinteza i biološka evaluacija nekih pirimidina, pirimido[2,1-b][1,3]tiazina i tiazolo[3,2-a]pirimidin derivata

4,6-Diamino-1H-pyrimidine-2-thione (1) was used for the preparation of the pyrimidine derivatives 2-5. Compound 5 was cyclized to produce pyrimido[2,1-b][1,3]thiazine derivatives 6, which was condensed with p-chlorobenzaldehyde to give compound 7. The latter compound was reacted with hydroxylamine to give isoxazolo[4,5-d]thiazino[2,3-a]pyrimidines 8. Compound 8b was treated with 2-chloroethyl methyl ether to afford compound 9. Similarly, compound 3 was reacted with chloroacetic acid to give thiazolo[3,2-a]pyrimidine 10, which was condensed with p-chlorobenzaldehyde to give compound 11. Compound 11 was condensed with hydroxylamine to give isoxazolo[4,5-d]thiazolo[2,3-a]pyrimidine 12. Compound 12b was treated with 2-chloroethyl methyl ether to afford compound 13. The biological evaluation of some prepared products showed that many of them revealed promising antimicrobial activity.4,6-Diamino-1H-pirimidin-2-tion (1) upotrebljen je kao ishodni spoj u sintezi derivata pirimidina 2-5. Spoj 5 je cikliziran u pirimido[2,1-b][1,3]tiazin derivat 6, koji je kondenziran s p-klorbenzaldehidom u spoj 7. Produkt 7 je u reakciji s hidroksilaminom dao izoksazol[4,5-d]tiazino[2,3-a]pirimidin 8. Spoj 8b je u reakciji s 2-kloretil metil eterom dao spoj 9. Slično je spoj 3 reagirao s kloroctenom kiselinom i dao tiazol[3,2-a]pirimidin 10, koji je kondenziran s p-klorbenzaldehidom u produkt 11. Spoj 11 je kondenzacijom s hidroksilaminom dao izoksazol[4,5-d]tiazolo[2,3-a]pirimidin 12. Spoj 12b je s 2-kloretil metil eterom dao produkt 13. Biološka evaluacija pokazuje da neki od sintetiziranih produkata imaju antimikrobno djelovanje

Sinteza i antimikrobno djelovanje fuzioniranih heterocikličkih pirola

Pyrrole derivatives 1a,b were used as precursors for the preparation of pyrrolo[2,3-d]pyrimidine derivatives 2a,b-7a,b. Also, the formation and structure of different pyrrolotriazolopyrimidine derivatives 8a,b-11a,b were discussed. Some of the prepared products showed potent antimicrobial activity.Pirolni derivati 1a,b upotrebljeni su kao prekursori za pripravu derivata pirolo2,3-dpirimidina 2a,b7a,b. Diskutirano je i nastajanje i struktura različitih derivata pirolotriazolopirimidina 8a,b11a,b. Neki od sintetiziranih spojeva posjeduju izraženo antimikrobno djelovanje

Trimethoprim-sulfamethoxazole in cyst fluid from autosomal dominant polycystic kidneys

Trimethoprim-sulfamethoxazole in cyst fluid from autosomal dominant polycystic kidneys. Cyst infection in patients with autosomal-dominant polycystic kidney disease (ADPKD) is often refractory to therapy, in part because of the limited entry of commonly used antibiotics into cyst fluid. To study the efficacy of trimethoprim-sulfamethoxazole in cyst infection, cyst fluid was obtained by percutaneous aspiration or at surgery from eight patients with ADPKD receiving trimethoprim-sulfamethoxazole. Cysts were categorized as nongradient or gradient by cyst-fluid sodium concentration. Trimethoprim-sulfamethoxazole concentrations within cysts were determined and cyst fluid inhibitory and bactericidal titers were assessed in vitro against Escherichia coli, Proteus mirabilis and Streptococcus fecalis. The mean cyst fluid trimethoprim and sulfamethoxazole concentrations were 15.2 µg/ml and 42.5 µg/ml, respectively. Preferential accumulation of trimethoprim was observed in gradient cysts, exceeding serum levels more than eightfold. Sulfamethoxazole penetrated cysts to a lesser extent, with. concentrations ranging from 10 to 70 percent of the serum level. Cyst fluid sampled prior to trimethoprim-sulfamethoxazole administration (control) demonstrated no antibacterial activity, while cyst fluid inhibitory and bactericidal titers following antibiotic administration were 1:32 or greater in most instances. These studies indicate that trimethoprim-sulfamethoxazole is likely to be efficacious in the treatment of cyst infection in polycystic kidneys

Production, characterization and anticancer activity of <em>Candida bombicola</em> sophorolipids by means of solid state fermentation of sunflower oil cake and soybean oil

The production of sophorolipids by <em>Candida bombicola</em> NRRL Y- 17069 grown in a mixture of sunflower oil cake and crude soybean oil as economic substrates with different fermentation techniques was studied. The highest yield (49.5 g·100 g⁻¹ substrates) was obtained from solid state fermentation after employing a new concept for extraction by methanol (E I) followed by ethyl acetate (E II), then partially purified with hexane (E III). The course of time of fermentation was also studied, and E I extracted of the 12^th day showed the minimum surface tension (45 mN·m⁻¹) at a critical micelle dilution (CMD) of 10% concentration. The produced sophorolipids were characterized and confirmed by FTIR and ¹H NMR spectroscopy. The anticancer activity of the produced compounds was assessed against MCF-7, HepG2, A549, HCT116 cancer cell lines and the results revealed that E III and E IV (a mixture of E I & E III) act as promising anticancer agents in HepG2 and A549 by inhibiting urokinase and histone deacetylase activities.<br><br>Se estudió la producción de soforolípidos por <em>Candida bombicola</em> NRRL Y- 17069 cultiva con diferentes técnicas de fermentación en una mezcla de torta de girasol y aceite de soja crudo, como sustratos económicos. El rendimiento más alto (49,5 g·100 g⁻¹ de sustrato) se obtuvo por fermentación en estado sólido después de extraer con metanol (IE) seguido de acetato de etilo (EII), y de purificación parcial con hexano (EIII). También se estudió el tiempo de fermentación, considerando que el extracto IE de 12 días mostró una tensión superficial mínima (45 mN·m⁻¹) a una dilución micelar crítica (CMD) de concentración 10 %. Los soforolípidos producidos se caracterizaron y se confirmaron mediante espectroscopia FTIR y RMN de ¹H. La actividad anticancerígena de los compuestos producidos se evaluó en células MCF-7, HepG2, A549, líneas celulares de cáncer de HCT116 y los resultados revelaron que EIII y EIV (una mezcla de EI y EIII) actúan como prometedores agentes anticancerígenos en HepG2 y A549 inhibiendo las actividades de uroquinasa e histona desacetilasa

Producción, caracterización y actividad anticancerígena de soforolípidos producidos mediante fermentación en estado sólido con Candida bombicola de tortas de girasol y aceite de soja

The production of sophorolipids by Candida bombicola NRRL Y- 17069 grown in a mixture of sunflower oil cake and crude soybean oil as economic substrates with different fermentation techniques was studied. The highest yield (49.5 g·100 g−1 substrates) was obtained from solid state fermentation after employing a new concept for extraction by methanol (E I) followed by ethyl acetate (E II), then partially purified with hexane (E III). The course of time of fermentation was also studied, and E I extracted of the 12th day showed the minimum surface tension (45 mN·m−1) at a critical micelle dilution (CMD) of 10% concentration. The produced sophorolipids were characterized and confirmed by FTIR and 1H NMR spectroscopy. The anticancer activity of the produced compounds was assessed against MCF-7, HepG2, A549, HCT116 cancer cell lines and the results revealed that E III and E IV (a mixture of E I & E III) act as promising anticancer agents in HepG2 and A549 by inhibiting urokinase and histone deacetylase activities.Se estudió la producción de soforolípidos por Candida bombicola NRRL Y- 17069 cultiva con diferentes técnicas de fermentación en una mezcla de torta de girasol y aceite de soja crudo, como sustratos económicos. El rendimiento más alto (49,5 g·100 g−1 de sustrato) se obtuvo por fermentación en estado sólido después de extraer con metanol (IE) seguido de acetato de etilo (EII), y de purificación parcial con hexano (EIII). También se estudió el tiempo de fermentación, considerando que el extracto IE de 12 días mostró una tensión superficial mínima (45 mN·m−1) a una dilución micelar crítica (CMD) de concentración 10 %. Los soforolípidos producidos se caracterizaron y se confirmaron mediante espectroscopia FTIR y RMN de 1H. La actividad anticancerígena de los compuestos producidos se evaluó en células MCF-7, HepG2, A549, líneas celulares de cáncer de HCT116 y los resultados revelaron que EIII y EIV (una mezcla de EI y EIII) actúan como prometedores agentes anticancerígenos en HepG2 y A549 inhibiendo las actividades de uroquinasa e histona desacetilasa

Rosenbluth Separation of the πᵒ Electroproduction Cross Section

We present deeply virtual πᵒ electroproduction cross-section measurements at xB = 0.36 and three different Q2 values ranging from 1.5 to 2 GeV2, obtained from Jefferson Lab Hall A experiment E07-007. The Rosenbluth technique is used to separate the longitudinal and transverse responses. Results demonstrate that the cross section is dominated by its transverse component and, thus, is far from the asymptotic limit predicted by perturbative quantum chromodynamics. Nonetheless, an indication of a nonzero longitudinal contribution is provided by the measured interference term σLT. Results are compared with several models based on the leading-twist approach of generalized parton distributions (GPDs). In particular, a fair agreement is obtained with models in which the scattering amplitude includes convolution terms of chiral-odd (transversity) GPDs of the nucleon with the twist-3 pion distribution amplitude. This experiment, together with previous extensive unseparated measurements, provides strong support to the exciting idea that transversity GPDs can be accessed via neutral pion electroproduction in the high-Q2 regime

Heavy metals concentrations and speciation of Pb and Ni in airborne particulate matter over two residential sites in Greater Cairo - reflection from synchrotron radiation

Synchrotron radiation-based techniques [X-ray absorption near-edge structure (XANES) and X-ray fluorescence (XRF)] combined with inductively coupled plasma-mass spectrometry (ICP-MS) were used for the assessment of heavy metals concentrations as well as lead (Pb) and nickel (Ni) speciation in airborne particulate matter (PM10) over two residential sites in Greater Cairo. Nineteen 24 h high-volume samples collected at Giza (G) Square and Helwan (H) University (Egypt) were selected for this study. Mean concentrations of heavy metals in PM10 at both sites were found to have the same descending order of Pb &gt; Cu &gt; Ni &gt; Cd &gt; Co &gt; As, of which concentrations of Pb, Cu, Ni and Cd in H samples were higher than those in G samples. For Pb, synchrotron-based XRF results were in good agreement with concentrations obtained by ICP-MS. The XANES spectra of PM10 at the Pb L 2-edge and Ni K-edge were compared with those of Pb and Ni in model standard compounds to provide information on the potential oxidation states as well as the chemical forms of those elements. The data show that Pb has similar chemical environments in both series G and H with the predominance of Pb2+oxidation state. Nickel was found as Ni(OH)2, NiO and Ni metal in the analyzed samples. However, the content of Ni in the background filter shows a very strong interference with that of the collected PM10. Carcinogenic and non-carcinogenic risks resulting from the inhalation of the studied heavy metals were assessed for children and adult residents and were found below the safe limits, at both sites