Search

Copyright of Journal of Agricultural Sciences, Belgrade is the property of University of Belgrade, Faculty of Agriculture and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Journal of Agriculture & Nature / Kahramanmaraş Sütçü İmam Üniversitesi Tarım & Doğa Dergisi is the property of Kahramanmaras Sutcu Imam Universitesi and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Erzincan University Journal of Science & Technology is the property of Erzincan Binali Yildirim Universitesi and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Journal of Faculty of Pharmacy of Ankara University / Ankara Üniversitesi Eczacilik Fakültesi Dergisi is the property of Ankara University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

(1) Background: Liver fibrosis is currently one of the top ten causes of death worldwide. Stem cells transplantation using mesenchymal stem cells (MSCs) is an alternative therapy which is used in the place of organ transplant, due to the incapacity of stem cells to endure oxidative stress in the damage site, thus affecting the healing process. The present study aimed to enhance the therapeutic potential of MSCs using combined therapy, along with the novel synthetic compounds of benzimidazol derivatives. (2) Methods: Eighteen compound series (benzimidazol derivatives) were screened against liver fibrosis using an in vitro CCl4-induced injury model on cultured hepatocytes. IC50 values were calculated on the bases of LDH assay and cell viability assay. (3) Results: Among the eighteen compounds, compounds (10), (14) and (18) were selected on the basis of IC50 value, and compound (10) was the most potent and had the lowest IC50 value in the LDH assay (8.399   ±   0.23 uM) and cell viability assay (4.73   ±   0.37 uM). Next, these compounds were combined with MSCs using an in vitro hepatocytes injury culture and in vivo rat fibrotic model. The effect of the MSCs + compounds treatment on injured hepatocytes was evaluated using LDH assay, cell viability assay, GSH assay and real-time PCR analysis and immuno-staining for caspase-3. Significant reductions in LDH level, caspase-3 and apoptotic marker genes were noted in MSCs + compounds-treated injured hepatocytes. In vivo data also showed the increased homing of the MSCs, along with compounds after transplantation. Real-time PCR analysis and TUNEL assay results also support our study. (4) Conclusions: It was concluded that compounds (10), (14) and (18) can be used in combination with MSCs to reduce liver fibrosis. [ABSTRACT FROM AUTHOR]

In our study, some benzimidazole-thiadiazole derivative compounds were designed to develop new anticancer drugs, and their structures were proven by 1H-NMR, 13C-NMR, and elemental analysis spectral data. The cytotoxic activities of the compounds were evaluated by comparing the reference compound fluorouracil using the MTT method on the HT29 cell line. In addition, the cytotoxic effect of the compounds against the L929 (healthy mouse fibroblast cell) cell line was evaluated in order to determine the selectivity of the compounds. When the IC50 values of the compounds are examined, the structure of 5-(2-(2,6-dimethoxyphenyl)-1H-benz[d]imidazol-5(6)-yl)-Ncyclohexyl-1,3,4-thiadiazol-2-amine (BT-2) compound with an IC50 value of 34.13±2.48 μM showed comparable efficacy to the reference drug fluorouracil (12.84 ± 3.66 μM). It was determined that the cytotoxic effect of BT-2 compound on L929 healthy cell line was lower than the reference drug. These results are promising in terms of improving the anticancer effect of BT-2 compound. In addition, TAS and TOS of the compounds and antioxidant properties of the compounds were evaluated. The TOS value of the BT-2 compound appears to be comparable to the control drug. [ABSTRACT FROM AUTHOR]

Bu çalışmada [(η6-p-simen)Ru(L2)Cl]CI genel formülüne sahip olan biyoaktif benzimidazol aren rutenyum organometalik bileşiği, salisilaldehitin 2-(aminometil)benzimidazol dihidroklorür(ambm2.2HCI) bileşiği ile reaksiyona sokulmasının ardından, [Ru(p-simen)klorür]2 eklenmesi ile hazırlandı. Biyoaktif benzimidazol aren rutenyum organometalik bileşiği UV-VIS, IR, ESI-MS, 1H NMR, 13C NMR spektroskopisi teknikleriyle karakterize edildi. Bileşiğin, Diferansiyel termal analiz (DTA) ve Termogravimetrik analiz (TGA) teknikleri ile ölçümleri yapıldı, ölçüm verileri incelendi.

(1) Background: Liver fibrosis is currently one of the top ten causes of death worldwide. Stem cells transplantation using mesenchymal stem cells (MSCs) is an alternative therapy which is used in the place of organ transplant, due to the incapacity of stem cells to endure oxidative stress in the damage site, thus affecting the healing process. The present study aimed to enhance the therapeutic potential of MSCs using combined therapy, along with the novel synthetic compounds of benzimidazol derivatives. (2) Methods: Eighteen compound series (benzimidazol derivatives) were screened against liver fibrosis using an in vitro CCl4-induced injury model on cultured hepatocytes. IC50 values were calculated on the bases of LDH assay and cell viability assay. (3) Results: Among the eighteen compounds, compounds (10), (14) and (18) were selected on the basis of IC50 value, and compound (10) was the most potent and had the lowest IC50 value in the LDH assay (8.399 ± 0.23 uM) and cell viability assay (4.73 ± 0.37 uM). Next, these compounds were combined with MSCs using an in vitro hepatocytes injury culture and in vivo rat fibrotic model. The effect of the MSCs + compounds treatment on injured hepatocytes was evaluated using LDH assay, cell viability assay, GSH assay and real-time PCR analysis and immuno-staining for caspase-3. Significant reductions in LDH level, caspase-3 and apoptotic marker genes were noted in MSCs + compounds-treated injured hepatocytes. In vivo data also showed the increased homing of the MSCs, along with compounds after transplantation. Real-time PCR analysis and TUNEL assay results also support our study. (4) Conclusions: It was concluded that compounds (10), (14) and (18) can be used in combination with MSCs to reduce liver fibrosis.

Copyright of Al-Mustansiriyah Journal of Science is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

(Benzimidazol-2-yl)-7-hydroxycoumarin and N-(2-hydroxyphenyl)-7-hydroxycoumarin-3-carboxamide have been synthesized by the condensation of ethyl 7-hydroxycoumarin-3-carboxylate in acetic acid. Acetylation with acetic anhydride and halogenation with bromine in acetic acid's presence of the previous compounds has yielded the corresponding acetoxy and dibromo derivatives. The synthesized molecules that contain coumarin ring have been evaluated for their activities against breast cancer and they have shown good in vitro antiproliferative activities against a human breast cancer line (MCF-7). The results have shown that 3-(benzimidazol-2-yl)-7-acetoxycoumarin had a significant cytotoxic effect compared to the standard DOX (doxorubicin) drug. [ABSTRACT FROM AUTHOR]

Copyright of Academic Platform - Journal of Engineering & Science is the property of Akademik Platform and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Objectives: The in vitro antioxidant properties of some 2-(2-phenyl)-1H-benzo(d)imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were investigated in this study. Materials and Methods: The in vitro antioxidant activity of compounds 1-12 was explored by determination of rat liver microsomal nicotinamideadenine dinucleotide phosphate dependent inhibition on lipid peroxidation (LPO) levels and microsomal ethoxyresorufin O-deethylase (EROD) activity. Results: All synthesised compounds had LPO inhibitory activity (15-57%) except compound 6, which contains a thiophene ring. Almost all the compounds displayed slightly inhibitory activity (2-20%) on EROD. Conclusion: The most active compound, 3 bearing a p-bromophenyl substituent at the second position of the benzimidazole ring, caused 57% inhibition of LPO level, while butylated hydroxytoluene showed 65% inhibition. None of the synthesised compounds had a marked inhibitory effect on EROD activity. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Health Sciences / Sağlık Bilimleri Dergisi is the property of Erciyes Universitesi Saglik Bilimleri Dergisi and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

In this study, some new propargyl derivatives were synthesized considering potential monoamine oxidase-B (MAO-B) inhibition potency of propargyl moiety. In synthesis studies, 2-chlorobenzimidazole was reacted with propargyl bromide in the presence of NaH and compound 1 was obtained. Compound 1 was treated with various benzylamine derivatives and final products (2a-2c) were gained. Structures of obtained compounds were established by spectroscopic methods. Effects of the synthesized compounds against MAO enzymes were observed by using in-vitro fluorimetric method. Activity studies revealed that synthesis compounds inhibited MAO enzymes to different extends. [ABSTRACT FROM AUTHOR]

Six different heterocyclic compounds containing 1H-benzo[d]imidazole nuclei (S1-S6) were prepared in two steps and their structures were characterized using different spectroscopic methods. The synthesized heterocyclic compounds were tested against human cervix adenocarcinoma (HeLa) and human healthy lung (Beas-2B) cell lines. Cisplatin as a positive control drug was tested against the cervix cell line under the same conditions. Compound S4 was found to exhibit high cytotoxic activity against HeLa cell line (IC50: 3.72 ± 0.14 μM). In the last step of the study, color images of the cells interacted with the drug candidates were taken using confocal microscope. [ABSTRACT FROM AUTHOR]

The biological properties of silver complexes are well known but the studies about the enzyme inhibitory properties of them are very rare. On the other hand, it is known that one of the anticancer mechanisms of action of benzimidazole derivatives is enzyme inhibition. Therefore, in this study, five novel N-benzylbenzimidazole-silver(I) complexes were synthesized and fully characterized by ¹H NMR, 13C NMR, IR, mass spectroscopic methods and elemental analyses. The inhibitory properties of the synthesized complexes were tested on the activity of human carbonic anhydrase I - II and polyphenol oxidase, and it was observed that the complexes inhibited the activity of these enzymes with the IC50 values of 29.58-32.65 μM, 21.05-23.65 μM and 30.38-44.45 μM, respectively. We suggest that by also considering the low toxicity of silver compounds to human body at low concentrations, the evaluated complexes in this study are promising agents in the treatment of glaucoma and hyperpigmentation as carbonic anhydrase and polyphenol oxidase inhibitors. [ABSTRACT FROM AUTHOR]

Los inhibidores basados en heteroátomos de nitrógeno han mostrado ser uno de los productos químicos eficaces en la inhibición de la corrosión de metales. Este estudio fue llevado a cabo con la teoría de funcionales de la densidad (DFT), utilizando distintos niveles de cálculo. Diversas propuestas fueron evaluadas para estimar los niveles de energía de los orbitales moleculares de frontera (HOMO-LUMO) y su isodensidad. Dichos parámetros fueron considerados para determinar la parte nucleofílica y electrofílica de las moléculas. Finalmente, se llevó a cabo un análisis de la reactividad química con los parámetros de afinidad electrónica, el potencial de ionización, la dureza química y el índice de electrofilicidad; el objetivo fue determinar el efecto sobre la dureza química al cambiar la posición de los sustituyentes.

Current analysis standardized, adapted and detailed Egg Hatch Assay (EHA) to diagnose the resistance of gastrointestinal nematodes to albendazole in sheep. Three in vitro assays were undertaken at 24 and 48 h, by methodology prescribed by the EMBRAPA Practical Handbook, with negative control distilled water and DMSO at 0.75% and concentration at 600, 300, 150, 112.5, 75, 37.5, 18.75, 9.37 and 4.68 µg/mL and positive control albendazole 25.000 µg/mL. Plates were incubated in buffer with BOD and maintained at 28°C. After 24h and 48h of incubation, larvae had eclosion in negative control groups and also in groups treated with 112.5 µg/mL and 75 µg/mL, respectively. It was not possible to diagnose anti-helminth resistance in EET due to limiting variables, such as the lack of discriminating dose for albendazole. The standardization, adaptation and detailing were possible to diagnose anti-helminth resistance of nematodes to albendazole. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Faculty of Pharmacy of Ankara University / Ankara Üniversitesi Eczacilik Fakültesi Dergisi is the property of Ankara University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Twenty-eight compounds of the type N´-substituted-2-(5-nitroheterocyclic-2-yl)-3H-benzo[d]imidazole-5-carboxamide were obtained using as an oxidizing agent the nitrobenzene to obtain the benzimidazole scaffold, a modification of the Steglich esterification reaction was used to obtain the final compounds. The compounds were tested as potential inhibitors of the β-hematin formation in vitro, and in vivo were tested as antimalarial against mice infected by a strain of Plasmodium berghei ANKA sensitive to chloroquine. The survival time was increased by the compounds 3a and 4d to 17.00 ± 1.26 and 20.20 ± 1.95 days, while the progress of the infection was reduced to 4.02 ± 0.45 and 3.05 ± 0.09, respectively. The cytotoxic activity of all these compounds was assessed against Jurkat E6.1 and HL60 two human cancer cell line, and fresh human lymphocytes. Four compounds 4a, n and 5a, n showed enhanced cytotoxicity against Jurkat E6.1 and HL60 cell lines; fresh lymphocytes were not affected. Using flow cytometry, apoptotic cell death was observed at 24 h. The aforementioned compounds enhanced apoptosis both tumor cell lines decreasing cell survival by inhibiting autophagy. [ABSTRACT FROM AUTHOR]

El objetivo de la presente investigación fue determinar la respuesta de un inoculante con base en cepas de Bradyrhizobium japonicum a la adición de alginato, en presencia de los fungicidas Carbendazim® y Fludioxonil®, peletizados en semillas de soya. El experimento consistió de ocho tratamientos completamente al azar, con un arreglo factorial 3x2, con tres repeticiones por triplicado. La estimación de sobrevivencia bacteriana, como variable de respuesta, fue realizada en tres tiempos de secado: 0, 24 y 48 horas. Los datos fueron expresados como [Log10 UFC/mL]. Los resultados mostraron que los dos fungicidas reducen significativamente (p

Resumo A utilização de anti-helmínticos por longos períodos como principal medida de controle das parasitoses gastrintestinais de ruminantes levou a ineficácia aos levamisol, benzimidazóis e avermectinas. Este estudo descreve a atividade anti-helmíntica in vivo em populações naturais de nematoides trichostrongilídeos de caprinos. Foram selecionados 18 rebanhos provenientes dos biomas Caatinga (n=12) e Mata Atlântica (n=6), do Estado da Bahia, Brasil, criados em pastagens comunais em região semiárida. Grupos de oito a 10 animais foram tratados com albendazol (ABZ), ivermectina (IVM), levamisol (LEV), moxidectina (MOX) e closantel (CLOS). Os resultados do Teste de Redução da Contagem de Ovos nas Fezes indicaram resistência simultânea dos gêneros Haemonchus sp. e Trichostrongylus spp. para o ABZ, IVM, LEV, MOX e CLOS. As percentagens de eficácia variaram de 0-92%, 0-75%, 0-91%, 69-97% e 0-85% para o ABZ, IVM, LEV, MXD e CLOS, respectivamente, no bioma Caatinga e 0-59% para o ABZ e 9-59% para o IVM no bioma Mata Atlântica. Verificou-se nos rebanhos eficácia inferior a 95% para estes anti-helmínticos, com exceção de um único rebanho no qual a eficácia para MOX foi de 97%, o que sugere a presença de NGIs resistentes aos principais classes de anti-helmínticos em rebanhos caprinos destes biomas.

Objectives: Cancer is one of the leading causes of death throughout the world. Current therapy options suffer from the major limitations of side effects and drug resistance. Thus, continuing search for newer and safer anticancer drugs remains critically important. From this point of view, in the present study benzimidazole-hydrazone derivatives were synthesized by aiming at the identification of new chemical entities as potent anticancer agents. Material and methods: A series of 12 new compounds of 4-(5(6)-substituted-1H-benzimidazol-2-yl)-N′thiophen/furan-2-yl-methylene) benzohydrazide derivatives were synthesized. The structures of the obtained compounds were elucidated using by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. In vitro cytotoxic activity of the compounds against A549, MCF-7 and NIH/3T3 cell lines was evaluated by MTT assay. Results: Among the tested compounds, compound 3e showed higher cytotoxicity against MCF-7 human breast cancer cells when compared with cisplatin. Also, it has lower cytotoxicty against healthy cell line, NIH/3T3. Conclusions: It was determined that compound 3e showed inhibition towards MCF-7. Considering the substituent effect on cytotoxic activity, compound 3e bearing 2-methylthiophene has attracted attention with its higher anticancer activities. [ABSTRACT FROM AUTHOR]

Objectives: In this study, some novel 2-(2-phenyl)-1H-benzo[d]imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were designed and synthesized. Materials and Methods: Compounds 1-12 were obtained by condensing 2-(2-phenyl)-1H-benzo[d]imidazol-1-yl)acetohydrazide (III) with the corresponding aromatic aldehyde derivatives in the presence of catalytic amounts of hydrochloric acid in ethanol. Results: Following the structure elucidation, epidermal growth factor receptor kinase inhibitor activity was measured. The ADP-Glo™ kinase assay determines kinase activity based on the quantification of the amount of ADP produced during a kinase reaction. Conclusion: Almost all of the compounds' kinase inhibitor activities were rather limited. [ABSTRACT FROM AUTHOR]

In this study, two novel dichloro-(1-alkylimidazoline)-(p-cymene)ruthenium(II), 3 and dichloro-(1-alkylbenzimidazole)-(pcymene) ruthenium(II), 4 complexes have been synthesized and characterized by spectroscopic techniques. In vitro antioxidant activities of new metal complexes have been investigated by inhibition properties of 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (•OH) and superoxide (O2 -.) radicals. Additionally, total antioxidant activity of each metal complexes was also determined. It was found that total antioxidant activity and DPPH, hydroxyl and superoxide radicals scavenging activities of compound 3 are more efficient than compound 4. [ABSTRACT FROM AUTHOR]

Gray mold caused by Botrytis cinerea Pers. is one of the most important diseases of strawberry (Fragaria x ananassa Duch.), and fungicide resistance is a concern. The objective of this research was to evaluate the sensitivity of B. cinerea isolates to the fungicides iprodione and thiophanate-methyl in two strawberry-producing areas in Mexico. Sixty-two B. cinerea isolates collected from strawberry fruits from Maravatio Valley (MV) and Zamora-Jacona Valley (ZJ) in Michoacan, Mexico, were used to determine the sensitivity distribution based on mycelium growth (MG) and conidial germination (CG). Each monosporic isolate was grown in 4 plates containing media amended with 0, 0.1, 0.5, 1, 10, 50 and 100 mg mL-1 of iprodione and 0, 0.1, 10, 100, 1000 and 2000 mg mL-1 thiophanate-methyl, and the experiment was conducted twice. The effective concentration (EC50) that inhibits 50 % of mycelial growth and conidial germination was determined for each isolate-fungicide combination by fitting the log-logistic model to the data. Fungicide sensitivity distributions were illustrated by box plots and histograms, and compared by the Kolmogorov-Smirnov non-parametric test. For iprodione, there were significant differences between the sensitivity distributions (p£0.0001) of both of the sampling areas for mycelia. In MV, the median EC50 was 0.35 mg mL-1, while that of the ZJ isolates was 1.5 mg mL-1. There were no significant differences in the sensitivity distributions of CG (p=0.47) between producing areas for conidia (median EC50 = 3.73 mg mL-1). For thiophanate-methyl, the sensitivity distribution for mycelia was scattered and bimodal, with significant differences between the sampling areas (p£0.002). The median EC50 of MG was 3.11 mg mL-1 in MV, and 2000 mg mL-1 in ZJ. There were no significant differences between the sensitivity distributions from MV and ZJ in the conidial germination assay (p=0.13, Ks=1.17). The EC50 varied from 0.01 to >2000 mg mL-1 (median=2.01 mg mL-1). Resistance in B. cinerea to thiophanate-methyl and iprodione is widespread in strawberry-producing areas in Michoacan. [ABSTRACT FROM AUTHOR]

The synthesis, characterization and liquid crystalline properties of N4,N4′-bis((1 H-benzo[ d ]imidazol-2-yl)methyl)-3,3′-dimethyl-[1,1′-biphenyl]-4,4′-diamine and of their corresponding Mn(II), Fe(II), Ni (II), Cu(II), and Zn(II) complexes are described. The ligand and complexes have been characterized by elemental analysis, magnetic susceptibility measurements (µeff), conductometric measurements and Fourier Transform Infrared (FTIR), Nuclear Magnetic Resonance ( 1 H NMR), ( 13 C-NMR) and UV–Vis spectroscopy. Spectral investigations suggested octahedral coordination geometrical arrangement for M(II) complexes. The phase transition temperatures were detected by differential scanning calorimetry (DSC) analysis and the phases are confirmed by optical polarizing microscopy (POM). The DSC and POM supported the mesomorphic properties of the uncoordinated ligand in which the enantiotropic smectic phases were recorded. However, not all of their corresponding M(II) complexes are liquid crystal. [ABSTRACT FROM AUTHOR]

Benzodiazepines are used as anxyolytic, hypnotic, sedative and antidepressant drugs and to treat anxiety, insomnia, and epileptic seizures and show other types of biological activities. In this study, ten new 4(2)-(8-hydroxyquinolinil-5)-2(-4)-aryl-2,3-dihydro-1H-1,5-benzodiazepines and their rearrangement products, 2- substituted benzimidazoles, were synthesized from 1-aryl-3- (8-hydroxyquinolinil-5) propenone-1 (-3) and ophenylenediamine in methanol-triethylamine (1:1) solution. The reaction between the diamine and chalcones containing the 8-hydroxyquinoline fragment was carried out under mild conditions by base-catalysis amination of the β-enonic fragment of the chalcones followed by cyclocondensation. The structures of these compounds were studied by spectroscopic methods (IR and 1H-NMR) and their chelating properties were demonstrated. We calculated and discuss their theoretical biological activity, and the influence of metal quelation on the electron acceptor hydroxyquinolinic fragment on the electronic spectra. [ABSTRACT FROM AUTHOR]

The 'click synthesis' of some novel O-substituted oximes, 5a-5j, which contain heterocycle residues, as new analogs of β-adrenoceptor antagonists is described (Scheme 1). The synthesis of these compounds was achieved in four steps. The formation of (E)-2-(1H-benzo[d]imidazol-1-yl)-1-phenylethanone oxime, followed by their reaction with 2-(chloromethyl)oxirane, afforded mixture of oil compounds 3 and 4, which by a subsequent tetra-n-butylammonium bromide (TBAB)-catalyzed reaction with N-H heterocycle compounds (Scheme 1), led to the target compounds 5a-5j in good yields. [ABSTRACT FROM AUTHOR]

Objective: Mutagenicity is an undesirable side effect of clinically prescribed drugs, thus raises the question of their potential carcinogenicity. Taking into account that nitro compounds are known for their genotoxicity, it will be considerable interest to assess the genotoxic activities of the benzimidazole/thiazolidinedione retinoid derivatives. For this reason, the present study reports the genotoxicity of previously synthesized benzimidazole/ thiazolidinedione-retinoid derivatives (Ates-Alagoz and Buyukbingol, 2001; Ates-Alagoz et. al., 2009) by the umu-microplate test system. Methods: In this study, since this derivates involve nitro groups, makes advantageous the use of the umu-test, using NM2009 and NM1011 strains especially designed for detecting the mutagenicity of nitro compounds. Two bacterial strains Salmonella typhimurium NM1011 and S. typhimurium NM2009, expressing high levels of nitroreductase (NR) and O-acetyltransferase (O-AT) respectively, were used in the tests. Chlorophenol red-β-D-galactopyranoside (CPRG), O-nitrophenyl- β-D-galactopyranoside (ONPG) were used as substrate in the enzyme assays along with a well-known genotoxic nitro compound, 4-nitroquinoline 1-oxide (4NQO), as the positive control in the test. Results: Benzimidazole/ thiazolidinedione-retinoids that contain NO2 group with different position on benzene ring showed no genotoxicity in both strains with both substrates. However, using CPRG as the colorimetric substrate resulted in stronger activity than using ONPG in test conducted in both strains with all compounds. Although the β-galactosidase activities with using CPRG were three fold higher than ONPG, parallel results were obtained for both substrates and strains with all compounds tested. For all compounds, the induction of umuC gene expression was found to be almost the same for the strains that overexpress nitroreductase and O-acetyltransferase. Conclusion: None of the derivatives showed genotoxic effects, a very important data, making them a potential drug candidate. [ABSTRACT FROM AUTHOR]

This study was designed to investigate the effect of fasting on the plasma disposition of albendazole (ABZ) in goats following oral administration. A total of 10 goats, aged 5-6 months were used in this study. The animals were allocated into two groups (fasted and fed groups) of five animals each. ABZ was administered orally to animals in two groups at 10 mg/kg bodyweight. Heparinize blood samples were collected between 1 h and 144 h after treatment and the plasma samples were analysed by high performance liquid chromatography for ABZ, active albendazole sulphoxide (ABZSO) and inactive albendazole sulphone (ABZSCh) metabolites. ABZ is not detected and ABZSO and ABZS02 metabolites were present in the samples of fed and fasted animals. Feeding was significantly enhanced the plasma concentration of the ABZSO and ABZSO2 metabolites. The area under the curve (AUC) and half-life (tl/2) of both metabolites were significantly larger and longer in fed compared to fasted animals, respectively. Moreover the maximum plasma concentration (Cmax: 1.06±0.17 µg/ml) of ABZSO2 was also significantly higher in fed group compared with the fasting group (0.72+0.20 µg/ml). The changes in plasma kinetics, reflecting an altered quantitative gastrointestinal absorption or metabolism, were reflected in increased availability of ABZ metabolites in the plasma of fed goats. This could be a strategy to extend the exposure of parasites to the more active metabolite of ABZ and thus to improve the efficacy in goats. [ABSTRACT FROM AUTHOR]

Copyright of Pesquisa Veterinaria Brasileira is the property of Colegio Brasileiro de Patologia Animal - CBPA and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

In the current work, new benzimidazole-based acetamide derivatives (2a-u) were synthesized and screened for their in vitro antimicrobial activity. Among these derivatives, compounds 2b-2g were found to be the most promising antibacterial agents against Pseudomonas aeruginosa. These compounds and streptomycin exhibited the same level of antibacterial activity with a MIC value of 125 µg/mL. Compounds 2p, 2s, 2t and 2u were the most potent antifungal derivatives against Candida krusei with a MIC value of 125 µg/mL when compared with ketoconazole (MIC= 62.5 µg/mL). Compounds 2s and 2u also exhibited the highest inhibitory activity against Fusarium solani with a MIC value of 125 µg/mL, whereas ketoconazole showed its antifungal activity with a MIC value of 62.5 µg/mL. [ABSTRACT FROM AUTHOR]

Purpose: The synthesis of eight new benzimidazole derivatives bearing dithiocarbamate moiety and subsequently their anticholinesterase activity evaluations were aimed in this present study. Material and Methods: 2-Bromoacetylbenzimidazole react with dithiocarbamate salt derivatives and the resulted compounds were elucidated by 1H NMR, mass spectral data, and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) in vitro by using a modification of Ellman's spectrophotometric method. Results: The new compound 1-methyl-2{2'[(N,Ndimethylaminothiocarbamoylthio)-acetyl]}benzimidazole (2b) can be identified as promising anticholinesterase agent in vitro due to its moderate inhibition effect, which is about 37%, when compared with standard substance Donepezil under the same experimental conditions. Conclusion: In comparing with the reference standard, among the synthesized eight new compounds the only compound namely 1-methyl-2{2'[(N,Ndimethylaminothiocarbamoyl-thio)-acetyl]}benzimidazole (2b) has a promising anticholinesterase activity. [ABSTRACT FROM AUTHOR]

Copyright of Chemical Industry / Hemijska Industrija is the property of Association of Chemical Engineers and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Abstract: 2-Anilino-4-(benzimidazol-2-yl)-pyrimidines, synthesized by reaction of a readily available benzimidazole-substituted enaminone with suitable arylguanidines, were shown to inhibit four cancer-related protein kinases (Aurora B, PLK1, FAK, and VEGF-R2). The most potent derivative exhibited antiproliferative activity for several cancer cell lines of the NCI in vitro cell line panel in submicromolar concentrations. Both the anilinopyrimidine structure and the substitution pattern at the aniline ring appear to be important for the protein kinase inhibitory activity. [Copyright &y& Elsevier]

To one pot synthesis of coumarins with benzimidazol or benzoxazol moieties, three different microwave irradiations based procedures are reported here which take place within a few minutes. In spite of fairly well yield of the products using solvent free procedures, 25-30% further yields were achieved within 3 minutes at 110 °C using 2 mL n-pentanol as solvent. [ABSTRACT FROM AUTHOR]

Coumarin-30 and its regioisomer 7-(diethylamino)-4-(1-methyl-1H-benzimidazol-2-yl)coumarin were synthesised utilising condensation of the corresponding formylcoumarin with N-methylphenylene-1,2-diamine as the key step. Furthermore, absorption and fluorescence emission spectra of the two coumarins were recorded. [ABSTRACT FROM AUTHOR]

The article focuses on a study that characterized the changes in the ovarian follicles on a comparative basis between normal anestrous (N) and lame anestrous (L) postpartum cows. The Dairy Farm of Punjab Agricultural University in Ludhiana, India was the site chosen for the study. Results of the study showed that there were no differences in the characteristics of the dominant follicle pertaining to growth, static and regressing phases and persistence in both cows. It also found that there is a tendency for a higher number of smaller follicles in L cows.

A novel protoberberine alkaloid, 13-hydroxyl gusanlung A (1), was isolated from the aerial parts of Gendarussa vulgaris Nees, along with 16 known compounds. The structures were elucidated on the basis of spectroscopic evidence or comparison with authentic samples. [ABSTRACT FROM AUTHOR]

Five Pt(II) complexes with the ligands 2-ethyl-/ or-benzyl-/ or-phenoxymethyl- and 1-methyl-2-hydroxymethyl- and 1-methyl-2-phenyl- benzimidazoles were synthesized and characterized by elemental analysis, and IR and 1H-NMR spectra and evaluated for their in vitro genotoxic activities by Rec-Assay test. Based on the data obtained in this study, the Pt(II) complexes tested might be taken into consideration as promising antitumor compounds. [ABSTRACT FROM AUTHOR]

SUMMARY1. More than 1300 different mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) cause cystic fibrosis (CF), a disease characterized by deficient epithelial Cl– secretion and enhanced Na+ absorption. The clinical course of the disease is determined by the progressive lung disease. Thus, novel approaches in pharmacotherapy are based primarily on correction of the ion transport defect in the airways. 2. The current therapeutic strategies try to counteract the deficiency in Cl– secretion and the enhanced Na+ absorption. A number of compounds have been identified, such as genistein and xanthine derivatives, which directly activate mutant CFTR. Other compounds may activate alternative Ca2+-activated Cl– channels or basolateral K+ channels, which supply the driving force for Cl– secretion. Apart from that, Na+ channel blockers, such as phenamil and benzamil, are being explored, which counteract the hyperabsorption of NaCl in CF airways. 3. Clinical trials are under way using purinergic compounds such as the P2Y2 receptor agonist INS365. Activation of P2Y2 receptors has been found to both activate Cl– secretion and inhibit Na+ absorption. 4. The ultimate goal is to recover Cl– channel activity of mutant CFTR by either enhancing synthesis and expression of the protein or by activating silent CFTR Cl– channels. Strategies combining these drugs with compounds facilitating Cl– secretion and inhibiting Na+ absorption in vivo may have the best chance to counteract the ion transport defect in cystic fibrosis. [ABSTRACT FROM AUTHOR]

Amaç: Bu çalışmada, ditiyokarbamat yapısı içeren benzimidazol türevlerinden sekiz yeni madde sentezlenmiş olup, in vitro koşullarda antikolinesteraz aktivitelerinin değerlendirilmesi amaçlanmıştır. Materyal ve Metod: 2-Bromoasetilbenzimidazol ve ditiyokarbamat türevlerinin reaksiyonu sonucu sentezlenen bileşiklerin yapıları 1H-NMR, kütle spektral verileri ayrıca elemental analiz ile aydınlatılmıştır. Ayrıca yapıları tayin edilmiş bileşiklerin Elmann"s spektrofotometrik yöntemiyle asetilkolin esteraz etkileri değerlendirilmiştir. Bulgular: Tüm bileşikler arasında 1-metil-2{2"[N,Ndimetilaminokarbamoyl-tio)asetil]}benzimidazol (2b) maddesi kayda değer in vitro antikolinesteraz aktivite göstermiştir. Referans madde olarak kullanılan Donepezil ile aynı koşullarda kıyaslandığında, 2b maddesi %37 oranında inhibe ettiği görülmüştür. Sonuç: Sentezlenen sekiz yeni bileşikten sadece (1-metil-2{2"[N,Ndimetilaminokarbamoyl-tio)asetil]}benzimidazol (2b) maddesi Donepezil ile kıyaslandığında, kayda değer in vitro antikolinesteraz aktiviteye sahip olduğu tespit edilmiştir.

Coumarin-7 and its isomer 4-(2-benzimidazolyl)-7-(diethylamino)coumarin were synthesised using condensation of the corresponding formylcoumarin with o-phenylenediamine as the key step. Moreover, absorption and fluorescence emission spectra of these two coumarins were recorded. [ABSTRACT FROM AUTHOR]

Copyright of Revista de Toxicología is the property of Asociacion Espanola de Toxicologia and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)