Mini Reviews in Medicinal Chemistry - Volume 6, Issue 11, 2006

Quinoxaline derivatives have received much attention in recent years owing to their both biological properties and pharmaceutical applications. In this review we focus the attention on quinoxalin-2(3)-ones and quinoxalin-2,3-diones. These derivatives are particularly interesting since some of them showed antimicrobial (against several bacteria, viruses, fungi, etc), or anticancer activities. Furthermore, others are reported to b Read More

This review summarizes the knowledge of the role of dietary PUFAs, especially ω-3, on normal brain function. Furthermore, it reports the evidence pointing to potential mechanisms of ω-3 fatty acids in development of neurological disorders and efficacy of their supplementation in terms of symptom management.

Adenosine-to-Inosine RNA editing introduces changes in RNA transcripts via a post-transcriptional mechanism, the hydrolytic deamination of adenosine (A) to inosine (I) which is interpreted as guanosine by cellular machineries. Adenosine deaminases that act on RNA (ADAR) enzymes catalyze editing in double-stranded (ds) RNA substrates.

The molecular scaffold is an oft-cited concept in medicinal chemistry suggesting that the definition of what makes a scaffold is rigorous and objective. However, this is far from the case with the definition of a scaffold being highly dependent on the particular viewpoint of a given scientist. It follows, therefore, that the definition of scaffold hopping and, more importantly, the detection of what constitutes a scaffold hop, is als Read More

The increasing drug resistance of malaria parasites against chemotherapeutics enforces new strategies in finding new drugs. Here, we describe a new class of compounds the piperidone 3-carboxylates which show an antiplasmodial effect in vitro and in vivo. This effect might be caused by inhibition of eukaryotic initiation factor (eIF-5A).

Adverse extracellular matrix (ECM) remodeling contributes to fibrotic disorders in the kidney, lung, and heart. Matrix metalloproteinases (MMPs) are key enzymes regulating ECM turnover, and MMP inhibition attenuates remodeling. Recent technological developments allow MMP-substrate relationships to be identified and explored as novel therapeutic targets. This review summarizes current and novel strategies to block MMP activity.

NKT cells are a subset of regulatory lymphocytes characterized by co-expression of the NK cell receptor- CD161 and an invariant TCR-α chain (Vα14-Jα28). They are most abundant in the liver, spleen, and bone marrow. NKT lymphocytes have been implicated in the regulation of autoimmune processes in both mice and humans. Activation of NKT lymphocytes leads to rapid amplification of either IFNγ or IL4, endo Read More

The transforming growth factor-β (TGF-β) superfamily includes TGF-β s, activin, myostatin and bone morphogenetic proteins. Misregulation of the activity of TGF-β family members is involved in pathogenesis of cancer, muscular dystrophy, obesity and bone and tooth remodeling. Natural inhibitors for the TGF-β superfamily regulate fine-tuning of activity of TGF-β family in vivo. In addition to natural inhibitors for the TGF-βf Read More

Chronic infection with hepatitis C virus (HCV) remains a global health concern. Using both in vitro and cellbased assays, a series of small molecule agents specific for the viral RNA-dependent RNA polymerase have been shown to interfere with viral RNA replication. Although no agents targeting this viral enzyme have demonstrated sustained efficacy in infected patients as measured by reduction in viral load at 72 weeks post-trea Read More

Nowadays, drug discovery based on a single-target-directed strategy seems inappropriate for the treatment of complex diseases that have multiple pathogenic factors. Recent research into new drugs, which are able to hit different targets, highlights the idea that a single molecule could be sufficient to treat multi-factorial diseases. In this review, examples of multi-target-directed compounds derived from lipoic acid are examined.

The pipeline for new antibacterials is bleak despite the fact that infectious diseases account for a quarter of all worldwide deaths due to disease. Bacteria are ideal organisms for a systems biology approach to understanding pathogenesis by combined use of genomic technologies and computer algorithms. This approach can be applied to identify control points in molecular networks, which could be targets for novel drugs.