Sinteza 1-acil-2-alkiltio-1,2,4-triazolobenzimidazola s antimikotskim, protuupalnim i analgetskim učinkom

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo[2,3-a]benzimidazole-2-thione intermediate reacted with one equivalent of the appropriate respective alkyl halide to give the corresponding 2-alkylthio derivative 3a-g. The latters were acylated to afford the 1-acyl-2-alkylthio-1,2,4-triazolo[2,3-a]-benzimidazole derivatives 4-10 in good yields. Structures of the new compounds were verified on the basis of spectral and elemental methods of analyses. Fourteen of the prepared compounds were tested for their possible antifungal activities. Most of the tested compounds showed activity against Candida albicans and Fusarium oxysporum comparable to that of fluconazole as a reference drug. Compounds 8a, 9a, and 10d are the most active ones against most of the used fungi. Compounds 3e, 4d, 5d, 6d, 7d, 8c, 8d, 9d, and 10d were tested for their anti-inflammatory and analgesic effects; most of these compounds showed potent and significant results compared to indomethacin. Moreover, ulcerogenicity and the median lethal dose (LD50) of the most active compound 8d were determined in mice; LD50 was found to be 275 mg kg-1 (i.p.).Sintetizirani su novi derivati 1,2,4-triazolo[2,3-a]benzimidazola reakcijom 1,2-diaminobenzimidazola s ugljičnim disulfidom. Nastali 1,2,4-triazolo[2,3-a]benzimidazol-2-tioni reagiraju s jednim ekvivalentom odgovarajućeg alkil halida pri čemu nastaju 2-alkiltio derivati 3a-g. Acilacijom produkata 3 dobiveni su derivati 1-acil-2-alkiltio-1,2,4-triazolo[2,3-a]-benzimidazola 4-10 u dobrim iskorištenjima. Strukture novih spojeva potvrđene su spektroskopskim metodama i elementarnom analizom. Ispitivano je antimikotsko djelovanje 14 priređenih spojeva, uz flukonazol kao poredbenu tvar. Većina testiranih spojeva djeluje na Candida albicans i Fusarium oxysporum slično kao flukonazol. Najaktivniji su bili spojevi 8a, 9a i 10d. Produkti 3e, 4c, 5c, 6c, 7c, 8b, 8c, 9c i 10c ispitani su na protuupalno i analgetsko djelovanje, uz indometacin kao poredbenu tvar. Većina spojeva ima značajno djelovanje. Najaktivniji spoj testiran je na ulcerogenost. Srednja letalna doza (LD50) određena je na miševima i iznosi 275 mg kg-1 (i.p.)

Heart diseases diagnosis using heart sounds

Heart sound is one of the oldest means for assessing the function of heart valves. It helps, together with echocardiograms and electrocardiographs, to give a clear and proper diagnosis of several diseases. Artificial neural networks are used to classify several valve-related heart disorders. A library of heart sound files, recorded via the traditional stethoscope, are used to extract relevant features using several signal processing tools, e.g., discrete wavelet transform (DWT), fast Fourier transform (FFT) and linear predictive coding (LPC). The achieved recognition rates were around 95.7%

Heart diseases diagnosis using HMM

The bare ear and the stethoscope were until recently of great help in classifying most heart diseases especially those related to valve problems. The newly developed electronic stethoscope and phonocardiography represent useful tools for recording heart sound signals. In this paper a diagnostic technique for heart diseases using heart sounds is suggested. Wavelet decomposition and mel cepstrum are used for feature extraction. Classification of the different heart diseases is then done using hidden Markov models (HMM). Three different techniques have been used and compared. The obtained recognition rates (RR) were 97.3%, 98.2%, and 99.1%

The Perceived Quality of University Climate Among King Khalid University Students in the Light of Some Demographic Variables

The current research aimed to identify the level of perceived quality of university climate among students at King Khalid University, and to explore the differences in perceived quality of university climate among students according to the variables: age group, gender, academic qualification, academic specialization, and participation in university activities. To achieve these aims; The descriptive method was used, and the researchers prepared and applied a perceived quality of university climate scale. The sample of the research consisted of (134) students (32 males and 102 females), their ages were between (18 – 45) years, they belonging to various programs at College of Education in King Khalid University. The research reached the following results: there was a moderate level of perceived quality of university climate scale and its sub-dimensions among King Khalid University students, and there were significant statistically differences in perceived university climate quality among students according to the variables: age group for adults, gender for males, participation in university activities for participants, and academic qualification for masters compared to bachelors, while there werent significant statistically differences in the level of perceived quality of university climate according to the variables of academic specialization and academic qualification (doctoral verse Master’s, and doctoral verse Bachelor’s)

The Citizenship Values Among Students at the College of Education in King Khalid University in the Light of Some Demographic Variables

The current research aimed to identify the level of citizenship values among students at the College of Education in King Khalid University, and to explore the differences in the citizenship values among students according to the variables: age, gender, academic qualification, academic specialization, and participation in university activities. To achieve these aims, the descriptive approach was used, and the researchers prepared and applied a citizenship values scale for university students. The sample of the research consisted of (134) students (32 males and 102 females), their ages were between (18 – 45) years, they belonging to various programs at College of Education in King Khalid University. The research reached the following results: there was a very high level of citizenship values and its three sub-dimensions among students, and there were no statistically significant differences in the citizenship values among students according to: age, gender, Academic qualification, and academic specialization. While there were statistically significant differences in the citizenship values among students according to participation in university activities for the participants in these activities

3-Ethyl-5-(4-meth­oxy­phen­oxy)-2-(pyridin-4-yl)-3H-imidazo[4,5-b]pyridine

In the title compound, C20H18N4O2, the imidazopyridine fused ring system is almost perpendicular to the benzene ring [dihedral angle = 87.6 (5)°]. The pyridine ring makes a dihedral angle of 35.5 (5)° with the mean plane of the imidazopyridine fragment. The crystal structure is stabilized by an aromatic π–π stacking inter­action between the phenyl rings of neighbouring mol­ecules [centroid–centroid distance = 3.772 (2) Å, inter­planar distance = 3.546 (2) Å and slippage = 1.286 (2) Å]

Effect of root-knot nematode and two species of crown gall on antioxidant activity of grape leaves

Agrobacterium tumefaciens and Agrobacterium vitis significantly reduced the entire criteria (galls, embedded stages, final population, Pf/Pi and egg production) of the root-knot nematode, Meloidogyne incognita, when they were in concomitance with grape (Vitis vinifera var) superior roots. Greater suppression in such criteria was observed with high inoculum levels (5X10 7 cfu/pot) than with lower (2.5X10 7 cfu/pot) ones. All treatments resulted in the increase of leaves contents of H 2 O 2 and lipid peroxidation (TBARS) dramatically, which were considered the most damaging stresses in plant cells. The contents of AsA, GSH, TPH and PAL specific activity increased as a strongly antioxidant defense compound against induced oxidative damage. In addition, the increase in the activity of various antioxidant defense specific enzymes (SOD, APX, CAT and GST) represented the protective activity used to counteract the oxidative injury promoted by nematode and nematode-bacteria infections. The rate of the chemical increase was significantly higher in interaction treatments than in the leaves of plants treated singly with M. incognita. Moreover, higher inoculum levels resulted in higher values of the measured chemicals. Symptoms appearance at low levels of nematode and bacterial treatments were significantly preceded by significant induction of AsA, GSH and TPH contents, and APX, CAT, SOD, GST and PAL activities in grape leaves. However, under high levels of nematode and bacteria, an obvious depletion at all non-antioxidants enzymes' levels and antioxidants enzymes' activities was observed. It is supposed that stimulated antioxidative processes contributed to the suppression of necrotic symptom development in grape leaves depending on the level of pathogen inoculum

Guidelines for the use and interpretation of assays for monitoring autophagy (4th edition)1.

In 2008, we published the first set of guidelines for standardizing research in autophagy. Since then, this topic has received increasing attention, and many scientists have entered the field. Our knowledge base and relevant new technologies have also been expanding. Thus, it is important to formulate on a regular basis updated guidelines for monitoring autophagy in different organisms. Despite numerous reviews, there continues to be confusion regarding acceptable methods to evaluate autophagy, especially in multicellular eukaryotes. Here, we present a set of guidelines for investigators to select and interpret methods to examine autophagy and related processes, and for reviewers to provide realistic and reasonable critiques of reports that are focused on these processes. These guidelines are not meant to be a dogmatic set of rules, because the appropriateness of any assay largely depends on the question being asked and the system being used. Moreover, no individual assay is perfect for every situation, calling for the use of multiple techniques to properly monitor autophagy in each experimental setting. Finally, several core components of the autophagy machinery have been implicated in distinct autophagic processes (canonical and noncanonical autophagy), implying that genetic approaches to block autophagy should rely on targeting two or more autophagy-related genes that ideally participate in distinct steps of the pathway. Along similar lines, because multiple proteins involved in autophagy also regulate other cellular pathways including apoptosis, not all of them can be used as a specific marker for bona fide autophagic responses. Here, we critically discuss current methods of assessing autophagy and the information they can, or cannot, provide. Our ultimate goal is to encourage intellectual and technical innovation in the field