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Bu çalışmada, antioksidan aktiviteye sahip bazı yeni heterosiklik oksadiazol türevlerinin sentezlenmesi amaçlanmıştır. 1,3,4-oksadiazoller, 4-metilfenilsülfonilhidrazidin farklı aromatik asitlerle POCl3 varlığında kondenzasyon reaksiyonu sonucu elde edilmiştir. Sentezlenen bileşiklerin yapıları 1H NMR ve 13C NMR spektroskopisi kullanılarak desteklenmiş ayrıca ince tabaka kromotografisi kullanılarak saflıkları kontrol edilmiştir. Elementel analizleri Carlo Erba 1106 elementel analiz cihazında yapılmıştır. 2,5-disübstitüye-1,3,4-oksadiazol türevlerinin (1-5) antioksidan aktiviteleri, ABTS (2,2′-Azino-bis(3-etilbenzenotiyazolin-6-sülfonik asid), DPPH (1,1-difenil-2-pikrilhidrazil) radikal giderme aktiviteleri ve demir indirgeme gücü antioksidan kapasitesine göre incelenmiştir. Elde edilen sonuçlar, sentezlenen bileşiklerin (1-5) etkili antioksidan aktiviteye sahip olduğunu göstermiştir.

A new series of 1,3-benzoxazol-2(3H)-one hybrid compounds, including coumarin, isatin 1,3,4-triazole and 1,3,4-thiadiazole moieties, were synthesized and biologically evaluated for their antioxidant capacities and anti-urease properties. The synthesized benzoxazole-coumarin (6a–e) and benzoxazole-isatin (10a–c) hybrids showed remarkable urease inhibitory activities with IC50 (μM), ranging from 0.0306 ± 0.0030 to 0.0402 ± 0.0030, while IC50 of standard thiourea is 0.5027 ± 0.0293. The synthesized benzoxazole-triazole (8a–c) and benzoxazole-thiadiazole (9a–c) hybrids showed similar urease inhibitory activities with IC50 (μM), ranging from 0.3861 ± 0.0379 to 0.5126 ± 0.0345. The antioxidant activity of the synthesized compounds was evaluated for their antioxidant activities, such as reducing power and ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt) radical scavenging. The results of ABTS radical scavenging activities of some of the synthesized molecules showed higher activities than standard Trolox, SC50 (μM) = 213.04 ± 18.12. One benzoxazole-coumarin (6f), two benzoxazole-isothiocyanate (7b, 7c), and two benzoxazole-triazole (8b, 8c) derivatives showed higher activities (SC50 (μM) values, 82.07 ± 10.34, 120.19 ± 7.30, 104.58 ± 10.55, 153.26 ± 7.14, and 144.82 ± 10.68, respectively) than standard Trolox, (SC50 (μM) = 213.04 ± 18.12). This work was supported by Research Fund of Recep Tayyip Erdogan University under the Project Number of FBA‐2018‐858.

The genus Inula belongs to family Asteraceae and it is medicinally important because it possesses cytotoxic, anticancer, hepatoprotective, antibacterial and anti-inflammatory properties. The aim of this research was to explore antioxidant and anti-urease activities of fifteen Inula taxa in Turkey. Ethanol extracts of Inula taxa were obtained by Soxhlet extraction. Antioxidant activity was determined through total antioxidant activity, total phenolic content and copper reducing antioxidant capacity (CUPRAC) analyses. The highest total phenolic content and total antioxidant capacity were found in I. orientalis (158.54?0.002 ?g GAE/mL) and I. macrocephala (189.16?0.002 ?g AAE/mL). CUPRAC activity increases with the increasing concentration of the extracts and the standard. Moreover, all the tested plants exhibited better anti-urease activity than standard thiourea except for I. anatolica and I. thapsoides subsp. thapsoides. Results obtained from this study demonstrate that Inula species might be utilized as a probable natural source in the pharmaceutical and food industries but further and more specific studies are needed to determine active antioxidative and anti-urease compounds in the extracts.

Background:Benzimidazoles and its derivatives have been attracting interest for many years because of their biological activities. Benzimidazoles containing different heterocyclic moieties have wide range of biological activities such as antimicrobial, antioxidant, anticancer, antiviral, etc.Methods:In this study, some benzimidazole derivatives containing furan, oxadiazole, triazole and thiadiazole moieties have been synthesized and then evaluated for their antioxidant and antiurease activities.Results:The results showed that all the tested benzimidazoles indicated remarkable urease inhibitory potentials with IC50 values ranging between 0.303±0.03 to 0.591±0.08 µM.Conclusion:In conclusion, synthesized benzimidazole derivatives showed good antioxidant and antiurease activities. Heterocyclic groups on benzimidazole nucleus enhance the activities.

WOS: 000479700000001 A novel series of N '-(substituted benzylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides and N '-(1-(substituted phenyl)ethylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides were synthesized and then studied for their urease inhibitory activities using thiourea as a standard drug. All newly synthesized compounds were found to exhibit potent inhibitory properties against urease enzyme in the range of IC50 = 0.0155 +/- 0.0039-0.0602 +/- 0.0071 mu M, when compared with the thiourea as standard (IC50 = 0.5115 +/- 0.0233 mu M). All target molecules were characterized by H-1-NMR, C-13-NMR, IR, and electrospray ionization mass spectrometry.

Many heterocyclic compound, a pharmacologically used as the starting compound for the synthesis of new structures which are important. Groups of these azole compounds, due to their various biological activities, in recent years have become common classes of compounds synthesized. Heterocyclic compounds containing five-membered ring, compounds of pharmacological class have entered popular in recent years due to properties. In this study, antioxidant activities of some 2,5-disubstitue-1,3,4-oxadiazoles (1-3) were evaluated for according to ABTS (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities and iron reducing power capacity. The obtained results showed that the synthesized compounds (1-3) had effective antioxidant activities.

İlk defa sentezlenmiş olan oksazolidinon türevi eperezolid benzeri bileşiklerin antiüreaz ve anti-elastaz aktiviteleri incelendi. En yüksek ve en düşük antiüreaz aktivite sırasıyla 8 (IC50 = 1.91x10-3 ± 2.97x10-4 μM) ve 10 bileşiklerinde (IC50 = 6,03x10-3±1,98x10-4 μM) gözlendi. En yüksek ve en düşük anti-elastaz aktivite ise sırasıyla 8 (IC50 = 2,2x10-2 ± 2,6x10-3 μM) ve 1 bileşiklerinde (IC50 = 4,1x10-2 ±1,3x10-3 μM) gözlendi.

Valproic acid (VPA) is an effective drug, which is preferred for the treatments of epilepsy and various kinds of seizures. Nonetheless, VPA has many life-threatening side effects associated with free radical production. Alpha-lipoic acid (ALA) is a powerful antioxidant, which can scavenge reactive oxygen species (ROS). The effects of ALA against VPA-stimulated brain injury were investigated. In this study, Sprague-Dawley rats were divided as four groups: Group I, control rats; Group II, ALA-administered rats (50 mg/kg/d); Group III, VPA-administered rats (0.5 g/kg/d); Group IV: VPA- and ALA-administered rats at the same dose and time. According to the results, VPA increased lipid peroxidation, protein carbonyl, advanced oxidation protein products, total oxidant status, nitric oxide levels and glutathione-S-transferase, adenosine deaminase, xanthine oxidase activities, decreased glutathione, total antioxidant capacity levels, catalase, superoxide dismutase, glutathione peroxidase, sodium-potassium ATPase, and paraoxonase activities. Treatment with ALA reversed these effects. In conclusion, we may suggest that ALA may be a good candidate for prevention of VPA-induced brain injury.

Tyrosinase (EC 1.14.18.1) is an enzyme containing copper that found in fungi, high plants and animals. Furthermore, it is catalyses there actions oxidation to o-quinones of o-diphenols and hydroxylation of monophenolsto o-diphenols using molecular oxygen. In this study, tyrosinase enzyme was purified for the first time from Kanlıca Mushroom (Lactarius salmonicolor) plenty of grown in Giresun Province and around and examined the kinetic properties. Optimum pH and temperature, pH and temperature stability, optimum reaction time, determining the optimum reaction time was the appropriate enzyme and substrate concentrations. The optimum pH of the purified tyrosinase from mushroom Kanlıca 6.0 was found to be optimal at 40ºC. The purified enzyme, which showed SDS-PAGE, had a molecular weight of 30 kDa.The Km and Vmax values of L. Salmonicolor tyrosinase toward were determined by Lineweaver Burk method., Tirozinaz (EC. 1.14.18.1) funguslarda, yüksek bitkilerde ve hayvanlarda bulunan; moleküler oksijenin etkisiyle monofenollerin o-difenollere hidroksilasyonu; o-difenollerin de o-kinonlara oksidasyon reaksiyonlarını katalizleyen ve bakır içeren bir enzimdir. Bu çalışmada, Giresun İli ve çevresinde bol miktarda yetişen Kanlıca Mantarından (Lactarius salmonicolor) tirozinaz enzimi ilk defa saflaştırıldı ve kinetik özellikleri incelendi. Optimum pH ve sıcaklık değerleri, pH ve sıcaklık stabiliteleri, optimum reaksiyon süresi, optimum reaksiyon süresinin tayini, uygun enzim ve substrat konsantrasyonu belirlendi. Kanlıca mantarından saflaştırılan tirozinazın optimum pH’sının 6,0; optimum sıcaklığının 40°C olduğu bulundu. SDS-PAGE elektroforezi sonucunda saflaştırılan enzimin molekül ağırlığının 30 kDa olduğu bulundu. L. Salmonicolor tirozinaz enziminin optimum pH ve sıcaklıkta L-tirozin substratı için Km ve Vmax değerleri Linewear-Burk yöntemi ile bulunmuştur.

Schiff bases have excellent characteristics, structural similarities with natural biological agents and synthetic flexibility. Schiff base-bimolecular condensation products with aldehydes of primary amines represent valuable intermediates in organic synthesis. Schiff bases derived from salicylaldehyde have been reported to have plant growth regulator, antimicrobial or antimycotic activity. In studies describing the relationship between quantitative structure-antitumor activity of a series of Schiff bases, Salicyldehydes have been shown to provide the best correlation in the ligands. In this study, 6 new Schiff bases were synthesized from the reaction of the substituted amino compounds with 5-bromosalicylaldehyde and their structures were illuminated spectroscopic data. The biological activities of this compound series were evaluated. The results show that the novel compounds synthesized have effective antioxidant and antiurease activities.

Bu çalışmada, ülkemizde Giresun İli ve çevresinde bol miktarda yetişen kestane (Castanea Sativa) tohumlarından lipaz enzimi ilk defa saflaştırıldı ve kinetik özellikleri incelendi. Petrol eteri ile yağı uzaklaştırılmış kestane tohumları 0,06 M sodyum fosfat tamponu (pH=7,0) ile homojenize edildi. Lipaz esteraz aktivitesi gösteren homojenizatın % 90’lık (NH4)2SO4 kesiti elde edildi. Dializden sonra bu kesit sırasıyla hidroksilapatit ve DEAE-selüloz kolonlara uygulanarak lipaz enzimi 186,87 kez saflaştırıldı. SDS-PAGE elektroforezi sonucunda saflaştırılan enzimin molekül ağırlığının 30 kDa olduğu bulundu. Kestane tohumlarından saflaştırılan lipazın optimum pH’sının 9,0; optimum sıcaklığının 30 °C olduğu bulundu. Enzimin çeşitli substratlara karşı ilgisi incelendiğinde, lipazın ilgisinin en çok p-NFM’a olduğu ve Km ve Vmax değerlerinin sırasıyla 1,017 mM ve 163,874 U olduğu saptandı.

WOS: 000444615600010 Lichens are complex associations composed of mycobiont and one or more algae or cyanobacteria which are living in symbiosis. Lichens are thought to possess therapeutic effects on many illnesses in worldwide. This study was performed to investigate antioxidant, anti-elastase and anti-urease activities of Usnea longissima Ach lichen. U. longissima was extracted with ethanol and ethyl acetate solvents. The antioxidant activities of the extracts of U. longissima were determined with methods such as 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical scavenging activity, copper reducing antioxidant capacity (CUPRAC), total antioxidant capacity, determination of total phenolic content and total flavonoid contents. The binding action of the DPPH and ABTS radicals, CUPRAC activity increases with concentration of the extracts. Ethanol extracts exhibited higher anti-urease and anti-elastase activity. Highest inhibition was found as 49.86% for elastase and 18.38% for urease. Results of the present study suggest that U. longissima extracts can be an alternative to synthetic antioxidant, anti-elastase and anti-urease agents. Giresun UniversityGiresun University [FEN-BAP-A-140316-62] This study was supported by Giresun University with the project number FEN-BAP-A-140316-62.

AKCAY, Hakki Turker/0000-0002-8502-9608 WOS: 000443574000012 In this study, the novel peripherally 4-[(2-methyl-1H-benzimidazol-1-yl)methoxy] substituted Zn(II) (3) Cu(II) (4), Co(II) (5) phthalocyanines were prepared and their structures were characterized spectro-scopically. The light absorption behaviors of the synthesized compounds (3-6) were studied by UV-Vis spectroscopy in the different concentration and different solvents were studied also. In addition, the urease inhibition activities of the synthesized compounds were also investigated. Among the synthesized molecules, compound 5 showed the best inhibitory effect against jack bean urease with IC50 values of 0.0034 +/- 0.0010 mu M. (C) 2018 Elsevier B.V. All rights reserved. Recep Tayyip Erdogan Universitesi - Research Funding [FBA-2017-788] This study was supported by Recep Tayyip Erdogan Universitesi - Research Funding - (Project no FBA-2017-788).

In this study, lipase enzyme was firstly purified from chamomile (Matricaria chamomilla L.) which is abundant inGiresun (Turkey) and surroundings and the kinetic properties of the enzyme were investigated. 70 % of (NH4)2SO4fraction of lipase esterase activity homogenate was obtained. After dialysis, this fraction was applied to DEAE-cellulosecolumn, and lipase was purified 26 times. In the purification process, the protein amount was determined by usingLowry and E280/E260 Warburg methods while lipase esterase activtiy was assayed with Erlanson’s method. It was foundthat the purified enzyme, which obtained with SDS-PAGE electroforesis, had a molecular weight of 30 kDa. Theoptimum pH and temperature values were determined. It was found that the lipase purified from chamomile had anoptimum pH value of 9 and an optimum temperature of 50 °C. When the affinity against different substrates of theenzyme was examined, the highest value was determined in p-nitrophenyl palmitate, with respectively Km and Vmaxvalues being 0.2899 mM and 144.93 Units. Also, the lipase enzyme purified from chamomile was immobilized onvarious carriers by adsorption, covalent and ionic binding methods. The kinetic properties of the immobilizedchamomile lipase such as optimum pH, optimum temperature were also studied., Bu çalışmada, Giresun İli ve çevresinde bol miktardayetişen papatyadan (Matricaria chamomillaL.) lipaz enzimi ilk defasaflaştırıldı ve kinetik özellikleri incelendi. Lipazesteraz aktivitesi gösteren homojenizatın % 70’lik (NH4)2SO4kesiti elde edildi. Dializden sonra bu kesit DEAE-selüloz kolonlara uygulanaraklipaz enzimi 26 kat saflaştırıldı. Saflaştırma işlemlerinde protein miktarıLowry ve E280/E260 Warburg yöntemlerine göre, lipazesteraz aktivitesi ise Erlanson yöntemine göre tayin edildi. SDS-PAGEelektroforezi ile elde edilen saflaştırılmış enzimin molekül ağırlığının 30 kDaolduğu bulundu. Optimum pH ve sıcaklık değerleri belirlendi. Papatyadansaflaştırılan lipazın optimum pH’sının 9, optimum sıcaklığının 50 °C olduğubulundu. Enzimin çeşitli substratlara karşı ilgisi incelendiğinde, lipazınilgisinin en çok p-nitrofenil palmitatta olduğu ve bu substrata karşı Kmve Vmax değerlerinin sırasıyla 0,2899 mM ve 144,93 Ünite olduğusaptandı.Ayrıca, papatyadan saflaştırılan lipaz enzimi çeşitlitaşıyıcılar üzerineadsorpsiyon, kovalent ve iyonik bağlama yöntemleri ile immobilize edildi. İmmobilizeedilmiş papatya lipazının optimum pH, optimum sıcaklık gibi kinetik özellikleride incelendi.

Bakteri ve mantar gibi mikroorganizmalar bitkilerde pek cok hastaliga yol acmaktadir. Patojenik mikroorganizmalarin cogu siklikla kullanilan antibiyotiklere ve sentetik fungisitlere direnc kazanmistir. Likenler bir mantar, bir alg veya bir siyanobakteriyum arasindaki simbiyotik birliklerdir. Likenler ve metabolitlerinin sentetik kimyasallara karsi umut vaat edici alternatifler olabilecekleri gosterilmistir. Bu calismanin amaci Cladonia stellaris , Cladonia pyxidata ve Cladonia furcata likenlerinin etil asetat ekstraktlarinin antibakteriyal etkisini ortaya koymaktir. Ekstraktlar sokslet ekstraksiyonu ile elde edilmistir. Antibakteriyal aktivite disk difuzyon metodu ile belirlenirken, antioksidan aktivite bakir indirgeme antioksidan kapasitesi (CUPRAC) metodu ile belirlenmistir. En iyi antibakteriyal aktivite C. stellaris ekstraktinda (25 mm) pozitif kontrol antibiyotiklerinden (ampisilin ve tetrasiklin) daha fazla olarak Pseudomonas syringae pv. syringae ve Erwinia carotovora subsp. c arotovora ’ya karsi bulunmustur. CUPRAC aktivitesi C. furcata > C. pyxidata > C. stellaris seklinde artmaktadir. Liken ekstraktlarindan aktif bilesenlerin izolasyonu ve bu bilesiklerin biyolojik aktivitelerinin belirlenmesinde daha ileri calismalar gerekmektedir.

Katalaz (E.C. 1.11.1.6), kararlı ve güçlü bir yükseltgen olan hidrojen peroksitin su ve moleküler oksijene dönüşümünü katalizleyerek parçalanmasını sağlayan enzimdir. Bu çalışmada, Giresun İli ve çevresinde yetişen Fındık Mantarı (Lactarius pyragalus)’ndan katalaz enzimi ilk defa saflaştırıldı ve kinetik özellikleri incelendi. Optimum pH ve sıcaklık değerleri, pH ve sıcaklık stabiliteleri, optimum reaksiyon süresi, optimum reaksiyon süresinin tayini, uygun enzim ve substrat konsantrasyonu belirlendi. Fındık mantarından saflaştırılan katalazın optimum pH’sının 8,0; optimum sıcaklığının 20 °C olduğu bulundu. SDS-PAGE elektroforezi sonucunda saflaştırılan enzimin molekül ağırlığının 30 kDa olduğu bulundu. Lactarius pyragalus katalaz enziminin optimum pH ve sıcaklıkta hidrojen peroksit (H2O2) substratı için Km ve Vmax değerleri Linewear-Burk yöntemi ile bulunmuştur. Km ve Vmax değerleri sırasıyla 0,310 mM ve 62,112 U olarak bulundu.

WOS: 000517086400001 A new series of benzimidazole derivatives (1-15) containing 1,2,4-triazole, 1,3,4-thiadiazole, 1,3,4-oxadiazole, and thiazolidinon rings have been synthesized. All new synthesized benzimidazole compounds were confirmed by H-1 NMR, C-13 NMR spectra, and LC-MS, and they were examined for their antioxidant and antimicrobial activities. Compounds 7 and 1 showed the highest and the lowest antioxidant activities, respectively. The lowest minimum inhibition concentration value found in compound 5 against Enterobacter aerogenes.

Lichens are a symbiotic association between a fungus and algaeand/or cyanobacteria. Lichen use as food and dye source, air pollutionindicator, medicinal and decoration. Inthis study, antimicrobial activity of ethyl acetate and ethanol extracts ofUsnea longissima Ach. lichen was searched by disc diffusion method. Whileinhibition zones ranges from 14.5 mm to 24.5 mm for bacteria, inhibition zonesranges from 10 mm to 32 mm for fungi. Lichen extracts exhibited higher activitythan gentamicinand tetracycline but they showed similar activity to nystatin. The MIC values of theextract varied between 0.002-0.117 mg/mL against bacteria; while The MIC valuesof the extract varied between 0.004-0.059 mg/mL against fungi. According to the obtainedresults, it could be said that U. longissima might be an alternative tosynthetic antimicrobial agents., Likenler bir mantar ve bir alg ve/ya da siyanobakteri arasındaki simbiyotikbirlikteliklerdir. Likenler besin ve boya kaynağı, hava kirliliği indikatörü,tıbbi ve dekorasyon amaçlı kullanılmaktadır. Bu çalışmada, Usnea longissimaAch. likeninin etanol ve etil asetat ekstraktlarının antimikrobiyalaktiviteleri disk difüzyon metodu ile araştırıldı. Bakteriler için inhibisyonzonları 14.5 mm ve 24.5 mm arasında değişirken; mantarlar için 10 mm ve 32 mmarasında değişmektedir. Liken ekstraktları gentamisin ve tetrasiklinden dahayüksek ve nistatine benzer aktivite göstermiştir. Ekstraktların bakterilerekarşı MİK değerleri 2-117 µg/mL arasında değişirken; mantarlara karşı MİKdeğerleri 4-59 µg/mL arasında değişmektedir. Elde edilen sonuçlara göre, U.longissima’nın sentetik antimikrobiyal ajanlara alternatif olabileceğisöylenebilir.

A series of Schiff base ligands containing 1,2,4-triazole ring were obtained by the addition of aldehydes to the amino compound under mild conditions in 80–82% yields. A reduction of these ligands with sodium borohydride resulted in Schiff base reduction products. New ligands were investigated for their antioxidant activities such as DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2’-azino-bis (3-ethylbenzo-thizoline-6-sulphonic acid) diammonium salt) radical scavenging and reducing power. 1H and 13C-NMR spectra (δ, ppm) were observed on a Varian Mercury 200 MHz spectrophotometer as standard substance using tetramethylsilane Match constants (J values) were given as Hertz. NMR coefficients are truncated as follows: s=singlet, d=dublet, t=triplet, m=multiplet signal. Combustion analysis was performed on a Carlo Erba 1106 elemental analyzer. All the compounds gave C, H, and N analysis results within ±0.6 % of the theoretical values. The IR spectra (υ, cm−1) were viewed with a Perkin-Elmer 1600 FTIR spectrometer in KBr pellets.

AKCAY, Hakki Turker/0000-0002-8502-9608 WOS: 000513010500102 PubMed: 31806475 In this study, novel peripherally 4-[(1H-benzimidazol-1-yl)methoxy] substituted Zn(II) (3) Cu(II) (4) and Co(II) (5) phthalocyanines were prepared and their structures were characterized spectroscopically. The light absorption behaviors of the synthesized compounds (3-5) were studied by UV-Vis spectroscopy at different concentrations in different solvents. The urease inhibition activities of the synthesized compounds were also investigated. Among the synthesized molecules, compound 4 showed the best inhibitory effect against jack bean urease with IC50 values of 0.0036 +/- 0.0010 mu M. (C) 2019 Elsevier B.V. All rights reserved. Recep Tayyip Erdogan Universitesi Research Funding [FBA-2017-788] This study was supported by Recep Tayyip Erdogan Universitesi Research Funding -(Project no FBA-2017-788).

In present study, the novel peripherally [3-methyl-5-oxo-4-(4-phenoxyphenyl)-4,5-dihydro-1H-1,2,4-triazol-1-yl] substituted Zn(II), Cu(II), Co(II) phthalocyanines were synthesized and characterized spectroscopically. The light absorption/emission behavior of the synthesized phthalocyanines were determined by UV-Vis and fluorescence spectroscopy. The fluorescence quantum yields of the novel phthalocyanine Zn(II) complex in different solvents were calculated. Besides, the urease inhibition activities of the novel compounds were investigated. All synthesized phthalocyanines have a superior inhibitory activity on urease enzyme, while novel phthalocyanines Cu(II) showed the best inhibitory effect against jack bean urease with IC50 values of 0.0035 ±0.0010 µM.

WOS: 000464108100016 PubMed: 30710848 A novel series of 5,6-dichloro-2-methyl-1H-benzimidazole derivatives was synthesized and then screened for their urease inhibitory activity. All compounds showed more potent inhibitory activity in the range of IC50= 0.0294 +/- 0.0015-0.1494 +/- 0.0041 mu M than thiourea (IC50= 0.5117 +/- 0.0159 mu M), as a reference inhibitor. Among all the tested compounds, the compound 15 (IC50= 0.0294 +/- 0.0015 mu M) having strong electron-withdrawing nitro group on the phenyl ring was recorded as the most potent inhibitor of urease. All compounds were docked at the active sites of the Jack bean urease enzyme to investigate the reason of the inhibitory activity and the possible binding interactions of enzyme-ligand complexes.

This work is aimed to assess of antioxidant and antifungal potential ofthe foliose lichen species: Flavoparmelia caperata, Xanthoparmelia stenophyllaand Xanthoparmelia conspersa. The antifungal activity of lichens were studiedagainst some pathogenic fungi by disc diffusion method. The acetonitrile extractsof these lichens were obtained with Soxhlet extraction. While F. caperataexhibited maximum antifungal activity (32 mm) against the C. albicans, theminimum antifungal activity (10 mm) was obtained from X. stenophylla lichenagainst S. cerevisiae. In CUPRAC assay, absorbance values was in order of BHTX.conspersaF. caperataX. stenophylla. As a result of the study, it was concludedthat these lichen species may be a potential source for the development of newantifungal and antioxidant compounds. Bu çalışma yapraksı liken türleri olan Flavoparmelia caperata,Xanthoparmelia stenophylla ve Xanthoparmelia conspersa’nın antioksidan veantifungal potansiyellerinin belirlenmesini amaçlamaktadır. Bu likenlerin bazıantifungal aktivitesi bazı patojenik mantarlara karşı antifungal aktivitesi diskdifüzyon metodu ile araştırılmıştır. Likenlerin asetonitril ekstraktları Soksaletekstraksiyonu ile elde edilmiştir. En yüksek antifungal aktivite (32 mm) F.caperata tarafından C. albicans’a karşı gözlenirken, en düşük antifungal aktivite(10 mm) X. stenophylla likeninden S. cerevisiae’ye karşı elde edilmiştir. CUPRACdeneyinde absorbans değerleri BHTX. conspersaF. caperataX. stenophyllaşeklinde sıralanmaktadır. Çalışma sonucunda, bu liken türlerinin yeni antifungalve antioksidan bileşik geliştirmede potansiyel bir kaynak olabilecekleri sonucunavarılmıştır.

Antioxidant is a defence mechanism in thehuman body preventing theoccurence of oxygen types and the damage generated by them. They are used forneutralizing free radicals. The presence of antioxidants activity indicates thepresence of the defense mechanism against the various diseases in the humanbody. Inthis study, activities of for the first time synthesized benzimidazolecompounds antioxidant activities are investigated spectrophotometrically. Theantioxidant activities of benzimidazole derivatives were investigated bydifferent antioxidant tests such as DPPH radical scavenging activity, ABTSradical scavenging activity and reducing power. All results were compared withsynthetic antioxidants such as BHT and Trolox. As theresult of the study, antioxidant activity level of the compounds especially 2, 5, 6a, 6b and 7b which are benzimidazole derivatives are found higher extent toothere compounds., Antioksidanlar, reaktif oksijen türlerinin oluşumunu ve bunların meydanagetirdiği hasarı önlemek için vücutta bulunan savunma mekanizmalarıdır. Serbestradikalleri nötralize etmek için kullanılırlar. Antioksidan aktivitesininvarlığı, vücutta meydana gelebilecek çeşitli hastalıklara karşı savunma mekanizmasınınvar olduğunu göstermektedir. Bu çalışmada, ilk defa sentezlenen benzimidazoltürevlerinin antioksidan aktiviteleri spektrofotometrik olarak incelendi.Benzimidazol türevlerinin antioksidan aktiviteleri, DPPH, ABTS radikal gidermeaktivitesi ve indirgeme gücü gibi çeşitli antioksidan testleri ile tayinedildi. Elde edilen sonuçlar, BHT ve Troloks gibi sentetik antioksidanlarlakarşılaştırıldı. Yapılançalışmalar sonucunda benzimidazol bileşiklerindenözellikle 2, 5, 6a, 6b ve 7b nolu bileşiklerin antioksidanaktivite değerleri diğer bileşiklere oranla daha yüksek bulundu.

yanardag, refiye/0000-0003-4185-4363 WOS: 000327494800009 PubMed: 24018846 Some series of arylidene barbiturates and thiobarbiturates were evaluated for their antibacterial, antioxidant, and urease inhibition activities. The arylidene barbiturates and thiobarbiturates were tested for antimicrobial activity using the agar well diffusion technique against 13 bacteria. The synthesized compounds (1a-g) were screened for antiurease and antioxidant activities. The results showed that the synthesized compounds (1a-g) had effective antiurease, antioxidant, and antibacterial activities.

yanardag, refiye/0000-0003-4185-4363 WOS: 000313663400009 PubMed: 22085138 The methoxy substitued two novel bis triazole-schiff bases (6 a-b) were synthesized with 4-amino-3,5-diethyl-4H-1,2,4-triazole and various bis-aldehydes. Their amine derivatives prepared by reduced with NaBH4 (5 a-b). The obtained products 6 a-b and 7 a-b were identified by FT-IR, H-1-NMR, C-13-NMR. The bis triazole-schiff bases and amine derivatives were tested for antimicrobial activity using the agar diffusion technique against 11 bacteria. The synthesized compounds (6 a-b and 7 a-b) were screened for their antielastase, antiurease and antioxidant activities. The resuts showed that the synthesized compounds (6 a-b and 7 a-b) had effective antielastase and antiurease activities.

Sahin, Huseyin/0000-0002-6018-1494 WOS: 000348103100007 PubMed: 25342259 The acylhydrazone compound named ethyl N'-furan-2-carbonylbenzohydrazonate was synthesized by the condensation of ethyl benzimidate hydrochloride with furan-2-carbohydrazide. The treatment of the acylhydrazone with hydrazine hydrate afforded 4-amino-3-furan-2-yl-5-phenyl-1,2,4-triazole. The usage of this compound with various aromatic aldehydes resulted in the formation of 4-arylidenamino-3-furan-2-yl-5-phenyl-1,2,4-triazoles. Sodium borohydride reduction of 4-arylidenamino derivatives afforded 4-alkylamino-3-furan-2-yl-5-phenyl-1,2,4-triazoles. The obtained products were identified by FT-IR, H-1-NMR, C-13-NMR. A series of compounds were evaluated for their antibacterial, antiurease, and antioxidant activities. The results showed that the synthesized new compounds had effective antiurease and antioxidant activities.

yanardag, refiye/0000-0003-4185-4363; Hasdemir, Belma/0000-0002-1071-1127 WOS: 000333246400017 PubMed: 24189917 A series of some 3-, 6-, 7-, 9-, 12-monohydroxy tetradecanoic acids were evaluated for their antiurease, antielastase and antioxidant activities for the first time in this study. All the test compounds exhibited antioxidant, antielastase and antiurease activities. The relationship between the position of the hydroxy group and the enzyme inhibition effect is studied in this work. The mentioned biological activities are depending on the position of hydroxy group of tetradecanoic acid isomers. The results obtained in this work are indicating that 3-, 6-, 7-, 9-, 12-monohydroxy tetradecanoic acid isomers can be used in agriculture, pharmacy and cosmetic industries due to their excellent antielastase, antiurease and antioxidant activities.

Gümüş, Arzu ( Balikesir Author ), A series of some 4-(aza substituted) methylene substituted dihydroxy coumarines were evaluated for their antioxidant and antielastase activities. Different in vitro methodologies such as total reducing power, 1,1-diphenyl-2-picrylhydrazil (DPPH.) free radical scavenging, ABTS radical scavenging activity were used as antioxidant activity. All the tested compounds exhibited potent free radical scavenging ability and antielastase activites., Giresun University - FEN-BAP-08/025

yanardag, refiye/0000-0003-4185-4363; TUNALI, SEVIM/0000-0003-3363-1290 WOS: 000309897100026 PubMed: 22889891 In this study, we aimed to investigate the effects of vitamin U (Vit U) on valproic acid (VPA)-induced liver damage. Female Sprague Dawley rats were randomly divided into four groups. Group I was intact control animals. Group If was control rats given Vit U (50 mg/kg/day) for fifteen days. Group III was given only VPA (500 mg/kg/day) for fifteen days. Group IV was given VPA + Vit U (in same dose and time). Vit U was given to rats by gavage and VPA was given intraperitoneally. On the 16th day of experiment, all the animals were fasted overnight and then sacrificed under ether anesthesia. Liver tissue was taken from animals, homogenized in 0.9% saline to make up to 10% homogenate. Liver aspartate and alanine transaminases, alkaline phosphatase, lactate dehydrogenase, myeloperoxidase, sorbitol dehydrogenase, glutamate dehydrogenase and xanthine oxidase activities and lipid peroxidation levels were increased and paraoxonase activity and glutathione levels were decreased in VPA group. Treatment with Vit U reversed these effects. These results demonstrated that administration of Vit U is a potentially beneficial agent to reduce the liver damage in VPA induced hepatotoxicity, probably by decreasing oxidative stress. (C) 2012 Elsevier Ltd. All rights reserved. Scientific Research Projects Coordination Unit of Istanbul UniversityIstanbul University [BYP-25257] This work was supported by Scientific Research Projects Coordination Unit of Istanbul University. Project number: BYP-25257.

yanardag, refiye/0000-0003-4185-4363 WOS: 000313663400011 PubMed: 22145614 A new bis schiffbases, 3 a-b were synthesized compound 2 with various bis aldehydes. Compounds 3 a-b have been reduced with NaBH4 to afford the corresponding bis amino triazole compounds 4 a-b. The obtained products 3 a-b and 4 a-b were identified by FTIR, H-1-NMR, C-13-NMR. A series of triazol derivatives were evaluated for their antibacterial, antioxidant, antiurease and antielastase activities. The results showed that the synthesized new bis-1,2,4-triazole derivatives had effective antioxidant, antiurease and antielastase activities.

Alpay Karaoglu, Sengul/0000-0003-1047-8350 WOS: 000320673200009 2-[6-(Morpholin-4-yl)pyridin-3-ylamino]acetohydrazide (4) was obtained starting from 6-morpholin-4-ylpyridin-3-amine (2) via the formation of ester (3) and then converted to the corresponding Schiff bases (5, 6) with the reaction with aromatic aldehydes. The carbothioamide (9), obtained from the reaction of hydrazide with phenylisothiocyanate, was converted to the corresponding 1,2,4-triazole (11) and 1,3,4-thiadiazole (12) derivatives by the treatment with NaOH or H2SO4, respectively. The cyclocondenzation of 9 with 4-chlorophenacyl bromide or ethyl bromoacetate produced the corresponding 1,3-thiazole (10) or 1,3-thiazolidine derivatives (13), respectively. Antimicrobial and antiurease activities of newly synthesized compounds were investigated. Some of them were found to be active on M. smegmatis, and they displayed activity toward C. albicans and S. cerevisiae in high concentration. Compound 10 proved to be the most potent showing an enzyme inhibition activity with an IC50 = 2.37 +/- A 0.19 mu M.

Tez (Yüksek lisans) -- Giresun Üniversitesi. Kaynakça var. x, 65 s. ; 27 cm. Demirbaş: 0063382 …

Bu çalışmada, ülkemizde Giresun İli ve çevresinde bol miktarda yetişen papatyadan (Matricaria chamomilla L.) ilk defa saflaştırılan lipaz enziminin çeşitli taşıyıcılara immobilizasyonu incelendi.Lipazlar (Triaçilgliserol açil hidrolaz, E.C.3.1.1.3), su-yağ ara yüzeyinde trigliseridlerin hidrolizini katalizleyen ve endüstride sayısız uygulama alanına sahip olan enzimlerdir. Gıda, deri, deterjan, kağıt, biyomedikal, biyodizel, biyosensör, kozmetik ve parfüm sanayinde uygulama alanları bulunmaktadır.Enzimlerin kimya endüstrisinde ve biyoteknolojide çeşitli amaçlar için kullanılması, bu katalizörlerin daha ekonomik ve kullanışlı hale getirilmesini gerektirmiştir. Endüstriyel işlemlerde immobilize lipaz enzimleri serbest lipaz enziminin yerini almış ve kullanım alanı artmıştır.Lipaz enziminin çok çeşitli bitkilerden saflaştırıldığı ancak papatya bitkisinden saflaştırılmadığı literatür araştırmalarından görülmüştür. Özgün nitelikte bir çalışma olduğu düşünüldüğünden, papatya bitkisinden lipaz enziminin ilk defa saflaştırılması ve çeşitli taşıyıcılara immobilize edilerek kullanım alanının arttırılması amaçlanmıştır. Enzimleri kimya ve biyoteknoloji alanında daha çekici hale getirebilmek için özellikle son 30 yıl içinde enzim immobilizasyonu üzerine çalışmalar yoğunlaşmıştır. İmmobilize enzimlerin endüstride, birçok alanda kullanımının yaygınlaştığı görülmektedir.Saflaştırılan lipaz çeşitli taşıyıcılar üzerine adsorpsiyon, kovalent ve iyonik bağlama yöntemleri ile immobilize edildi. Protein miktarı ve lipaz esteraz aktivitesi, sırasıyla Lowry ve Erlanson yöntemlerine göre tayin edildi.Papatya lipazı çeşitli taşıyıcılar (Kieselgel 60, deniz kumu, Amberlite IRA-900, alumina, cam boncuk) üzerine immobilize edilerek immobilize lipazların optimum pH, optimum sıcaklık, optimum reaksiyon süresinin tayini gibi kinetik özellikleri de incelendi. In this study, the immobilization of lipase enzyme, which has been purified for the first time, from chamomile (Matricaria chamomilla L.) grown in Giresun Province and its surroundings was investigated. Lipases (Triacylglycerol acyl hydrolase, E.C.3.1.1.3) are enzymes that catalyze the hydrolysis of triglycerides at the water-fat interface and have numerous applications in the industry. They have application areas in food, leather, detergent, paper, biomedical, biodiesel, biosensor, cosmetics and perfume industries.The use for various purposes in the chemical industry and in biotechnology of enzymes has necessitated making more economical and useful of these catalysts. In industrial processes, the immobilized lipase enzymes replaced of free lipase enzymes and increased its use. It was seen in literatüre studies that lipase enzyme has been purified from various plants but not purified from chamomile plants. Since it is thought to be an original work, it was aimed to purify from chamomile plant of lipase enzyme and increase its use by immobilizing to various carriers for the first time. In order to make enzymes more attractive in chemistry and biotechnology, studies on enzyme immobilization have intensified in the last 30 years. It is seen that the use of immobilized enzymes in industry in many fields has become widespread. The purified lipase was immobilized on the various carriers by adsorption, covalent and ionic bonding methods. Protein amount and lipase esterase activity were determined according to Lowry and Erlanson methods, respectively. Chamomile lipase was immobilized on various carriers (Kieselgel 60, sea sand, Amberlite IRA-900, alumina, glass beads) and it was investigated kinetic properties such as optimum pH, optimum temperature and optimum reaction time of immobilized lipases. 68

Tez (Yüksek lisans) -- Giresun Üniversitesi. Kaynakça var. xı , 84 s. : 28 cm. Demirbaş: 0063339 …