Current Medicinal Chemistry - Volume 20, Issue 30, 2013

Reactive oxygen species (ROS) are a group of highly reactive chemicals under tight control of intracellular antioxidants. The balance in oxidation-antioxidation is essential for maintaining normal cell functions, and any imbalance could lead to a wide range of diseases including cancer. The intracellular level of ROS is generally elevated in cancer cells, revealing a critical role of ROS in the process of carcinogenesis and cance Read More

In the panorama of HIV protease inhibitors (HIV PIs), many efforts have been devoted to the development of new compounds with reduced peptidic nature in order to improve pharmacokinetics and pharmacodynamics features. The introduction of cyclic scaffolds in the design of new chemical entities reduces flexibility and affords more rigid inhibitors. Specifically, common dipeptide isosteres are replaced by a central cyclic scaf Read More

The aim of this review is to highlight the advances in the field of heme oxygenase-1 (HO-1) inhibitors over the past years, particularly from a medicinal chemistry point of view; progresses made in the field strongly helped to clarify physiological roles of the heme oxygenase (HO) system. HO is a family of ubiquitously expressed enzymes which regulate the regiospecific catabolism of heme leading to the formation of equi Read More

Hepatitis C virus (HCV) infection is one of the main causes of liver disease worldwide. Its treatment is currently based on the combination of peg-interferon, ribavirin, and, for patients with genotype 1, a protease inhibitor (telaprevir or boceprevir). However, interferon-based combinations are not effective in all patients. Moreover, they are contraindicated in patients who cannot receive interferon (e.g. those with decompensate Read More

Sulfur (S), as the second element in the main group 6A just below oxygen (O), has been often used as an isosteric replacement for O in enzymatic mechanistic studies. In addition, S has also been used as an isosteric replacement for CH2. These S-based mechanistic probes have been used in the studies with protein enzyme systems such as the sirtuin family of the protein Nε-acyl-lysine deacylases, phosphotransferases, and fa Read More

Polymyxins are polypeptide antibiotics, with a primary effect of membrane damaging due to their selective binding to the lipopolysaccharide of Gram-negative bacteria. Their nephro- and neurotoxic side effects limited their use, however, in the last decade the emergence of multidrug-resistant Gram-negative bacteria led to the reintroduction of polymyxins into clinical practice. This review provides an overview about th Read More

Diabetic nephropathy (DN) is a major complication of diabetes and the leading cause of end-stage renal disease (ESRD). Approximately, one third of diabetic patients develop diabetic nephropathy. As diabetes and its associated metabolic diseases are becoming epidemic, DN is emerging as a major health threat to humans. Currently, there are no effective therapeutic treatments for the disease. As a result, most DN cases pro Read More

Tuberculosis (TB), an ongoing public health threat, is worsened by the emergence of drug resistance. With an estimated 630000 cases per year of multidrug resistant (MDR)-TB, and 9% of those being extensively drug resistant (XDR)-TB, there is an urgent need for new and more effective anti-TB drugs. New TB treatment regimens should be able to shorten the duration of therapy that currently takes at least six months. The no Read More

A methodology is described for the highly efficient and divergent synthesis of pseudosugars which allows the stereoselective introduction of polar groups at either the α or the β pseudoanomeric positions. Using this method, a series of 3-deoxycarbasugar analogues of mannose bearing a pyridyl group are rationally designed, prepared and tested for inhibition of Golgi α-mannosidase II.