Mini Reviews in Medicinal Chemistry - Volume 10, Issue 3, 2010

The InhA-related enoyl-ACP reductase, an enzyme involved in fatty acid synthesis, is one of the best validated targets for the development of anti-tubercular agents. However, the majority of isoniazid (INH)-resistant clinical strains are observed mainly due to the emergence of KatG mutants that do not form an INH-NAD adduct. Thus compounds that directly inhibit InhA avoiding activation by KatG would be promising candidat Read More

Magnetic iron oxide nanoparticles have attracted extensive interest as novel contrast agents for biomedical imaging owing to their capability of deep-tissue imaging, non-invasiveness and low toxicity. This mini-review will provide an overview on the recent synthesis methods, influencing factors and potential applications of magentic nanoparticles for cell labeling and imaging.

Niacin has broad spectrum lipid modifying and anti-atherosclerotic properties. It is the most effective medication available for raising raise high density lipoprotein (HDL) levels. Despite statin therapy there remains a considerable residual cardiovascular risk attributed to low HDL levels. Currently, statins decrease cardiovascular events and death by about 25-40%. Trials with surrogate endpoints have shown a decrease in Read More

The present review focused on the strategies aimed to possibly solve toxicity problems of distamycins. Distamycins are compounds characterized by an oligopeptidic pyrrolocarbamoyl frame ending with an amidino moiety. This class of compounds displays antiviral and antibiotic activity and shows interesting antiprotozoal activity related to the ability to reversibly bind to the minor groove of DNA with a high selectivity for TA-ri Read More

Elevated lipid level is supposed to be one of the main risk factors of atherosclerosis and related cardiovascular diseases and stroke (and is connected to mortality and morbidity). Therefore, lipid lowering is one of the major approaches in prevention of coronary heart diseases and stroke. Though drugs of various categories acting through different mechanisms are available in the antihyperlipidemic therapy, there a Read More

The first generation of in vitro models providing successful isolation of viable brain endothelial cells from different species, which could be maintained in cell culture, have emerged around thirty years ago. However, the time consuming and the difficulty of working with primary culture cells led to the development of simpler models employing cell lines with blood-brain barrier properties. The creation, in late nineties, of Read More