Mini Reviews in Medicinal Chemistry - Volume 10, Issue 9, 2010

The present mini-review highlights the recent developments on different classes of synthetic hybrids of natural and/or unnatural bioactive compounds, the utilization of which is very promising, as distinct features of each component can be hybridized and their properties leveraged. Particular stress is put on the respective mode of action and the corresponding rationale behind covalent combinations of various bioact Read More

Pyrrolidine scaffold has been widely used to design a variety of N-heterocyclic derivatives towards various targets. Amongst them, matrix metalloproteins (MMPs) and aminopeptidase N (APN) represent two kinds of important metalloproteinase targets which have been proved to be tightly related to tumor proliferation, invasion, metastasis and angiogenesis. As a result, their respective inhibitors, namely MMP inhibitor Read More

Synthetic nucleoside mimics are important candidates for antiviral and anticancer drugs. Ribavirin, the first antiviral nucleoside drug, is unique in its antiviral activity with mutilple modes of action, which are mainly due to its special triazole heterocycle as nucleobase. Additionally, introducing aromatic functionalities to the nucleobase is able to confer novel mechanisms of action for nucleoside mimics. With the aim to combine Read More

Certain xenobiotics are given in the “prodrug” form. Either the human body, or one compartment of the body, or the targeted virus itself metabolizes the prodrug into its active form. The bioprecursor form of drugs is used for a wide variety of reasons, namely: to make drug penetration into the target organ (mainly to the brain through the blood-brainbarrier) possible, eliminate unpleasant taste, alter (either i Read More

Endocrine-disrupting chemicals (EDCs) are a group of diversely natural compounds or synthetic chemicals that can interfere with the programming of normal endocrine-signalling pathways during pre- and neonatal life, thus leading to adverse consequences later in life. In addition, early life exposure to EDCs may alter gene expression and consequently transmit these effects to future generations.

Adiponectin is a collagen-like protein expressed in adipose tissue. Low serum adiponectin is associated with insulin resistance, atherogenic hyperlipidemia and arterial hypertension. High serum adiponectin predicted a reduced risk of myocardial infarction. Other surveys have shown that high levels of serum adiponectin were a predictor of future cardiovascular disease and mortality. These paradoxical findings might be ex Read More

Imaging the N-methyl-D-aspartate receptors (NMDARs) in the living human brain by positron emission tomography (PET) or single photon emission computed tomography (SPECT) would provide useful information on the role of these receptors in ischemia and in various neurological disorders such as degenerative diseases, epilepsy or schizophrenia. To assess NMDAR radiotracer development and to propose perspectives, we o Read More