Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy

The ruthenium complex,trans-[Ru(Bz)(NH3)(4)SO2](CF3SO3)(2) 1, Bz = benznidazole (N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide), is more hydrosoluble and more active (IC50try/1 h = 79 +/- 3 mu M) than free benznidazole 2 (IC50try/1 h > 1 mM). 1 also exhibits low acute toxicity in vitro (IC50macrophages > 1 mM) and in vivo (400 mu mol/kg < LD50 < 600 mu mol/kg) and the formation of hydroxylamine is more favorable in 1 than in 2 by 9.6 kcal/mol. In murine acute models of Chagas` disease, 1 was more active than 2 even when only one dose was administrated. Moreover, 1 at a thousand-fold smaller concentration than the considered optimal dose for 2 (385 mu mol/kg/day = 100 mg/kg/day), proved to be sufficient to protect all infected mice, eliminating the amastigotes in their hearts and skeletal muscles as observed in H&E micrographics.

Insights into the Molecular Requirements for the Anti-obesity Activity of a Series of CB1 Ligands

Two-dimensional and 3D quantitative structure-activity relationships studies were performed on a series of diarylpyridines that acts as cannabinoid receptor ligands by means of hologram quantitative structure-activity relationships and comparative molecular field analysis methods. The quantitative structure-activity relationships models were built using a data set of 52 CB1 ligands that can be used as anti-obesity agents. Significant correlation coefficients (hologram quantitative structure-activity relationships: r 2 = 0.91, q 2 = 0.78; comparative molecular field analysis: r 2 = 0.98, q 2 = 0.77) were obtained, indicating the potential of these 2D and 3D models for untested compounds. The models were then used to predict the potency of an external test set, and the predicted (calculated) values are in good agreement with the experimental results. The final quantitative structure-activity relationships models, along with the information obtained from 2D contribution maps and 3D contour maps, obtained in this study are useful tools for the design of novel CB1 ligands with improved anti-obesity potency.

Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: Anti-Mycobacterium tuberculosis activity and cytotoxicity

The aim of this study was to identify a candidate drug for the development of anti-tuberculosis therapy from previously synthesized compounds based on the thiosemicarbazones, semicarbazones, dithio-carbazates and hydrazide/hydrazones compounds. The minimal inhibitory concentration (MIC) of these compounds against Mycobacterium tuberculosis was determined. Their in vitro cytotoxicity to J774 cells (IC(50)) was determined to establish a selectivity index (SI) (SI = IC(50)/MIC). The best compounds were the thiosemicarbazones (2, 3 and 4) and the hydrazide/hydrazones (14, 15, 16 and 18). The results are comparable to or better than those of ""first line"" or ""second line"" drugs commonly used to treat TB, suggesting these compounds as anti-TB drug candidates. (C) 2010 Elsevier Masson SAS. All rights reserved.

Elitutbildning: en strategi för erkännande? : En studie om anti-diskrimineringsstrategier bland juriststudenter med ursprung i Mellanöstern

Elite Education: a strategy for recognition? A study on anti-discrimination strategies among law-students of Middle Eastern background While research show that individuals of foreign background are being discriminated against and stigmatized in Sweden, an increasing number of them still choose higher education and also show a tendency towards choosing an elite education. In this article, I examine if there is a link between experiences of discrimination and the choice of elite education. The study is based upon semi-structured interviews with five female and five male law students of Middle Eastern background. The findings show that discrimination, either against the students or their parents, has led to a high study motivation where the choice of elite education can be understood as an anti-discrimination strategy. Other anti-discrimination strategies are to resist a victim mentality and to destigmatize by challenging stereotypes. These anti-discrimination strategies can be understood as strategies for recognition, that is, striving for equality by being ascribed a positive status.

Постсекулярность и цифровой антиклерикализм в Рунете [Post-Secularity and Digital Anti-Clericalism on Runet]

This article deals with the phenomenon of “digital anti-clericalism” in the Russian-speaking sphere of the Internet (Runet). In the context of post-secularism the claims of Russian clerical and bureaucratic elites to the ideological monopoly in the political and social life face a strong resistance from the champions of religious pluralism and preservation of a secular state. Presented here is a detailed analysis of the topics and the stylistic features of different types of anti-clerical Internet communication – a variety of political folklore (memes, demotivators, photoshopped pictures). Also traced is the connection between the modern anti-clericalism on Runet and the late Soviet counter-culture. Suggested for the first time is a classification of anticlerical and atheist websites that constitute a vital part of the Russian blogosphere.

Teachers talking difference: teacher education and the poetics of anti-racism

This paper reports on a case study which explores the experiences of two teachers of ethnic difference working in secondary schools in rural Australia. In seeking an alternative way of telling their stories, transcript poems have been constructed from data obtained through semi-structured interviews with the teachers. The poems highlight the teachers' experiences of marginalisation and racism and their responses to their positioning in mainly white Anglo-Australian school communities. The study raises particular concerns about the effects of professional and cultural isolation on young and inexperienced teachers of ethnic difference as well as the need to view teacher education as an important site for the development of greater cultural awareness in "mainstream" teacher education students.

Kim's style guide for the kinaesthetic boffin: an exercise in anti-communication

The following article refers to a performed paper, Did the Paradigm Shift for You, Darling? given as a collaboration between John Cumming, Yoni Prior, David Ritchie and me at the Double Dialogues Conference, Lines of Flight, at Theatreworks in Melbourne, November, 1997. The performance involved the staging of a mock analysis of a section of my choreographic work, Kim’s Style Guide for the Kinaesthetic Boffin, by three fictitious ‘critics’. The performance functioned as an implicit critique of three different approaches to interpreting dance. This article explores a theoretical position which supports that critique.

The problem of voluntariness: parents and the anti-discrimination principle

Examines the theoretical justifications for the anti-discrimination protection for working parents in Australia. Implication of discrimination, voluntaries and employment; Analysis of the tort principles; Factors affecting the justification for protecting working parents.