Current Medicinal Chemistry - Volume 16, Issue 25, 2009

GEMSP is a mixture of functional polypeptides: fatty acids linked to poly-L-Lysine (PL), antioxidants linked to PL, free radical scavengers linked to PL, and amino acids linked to PL (patent numbers 6114388 (USA) and 792167 (EU)). In this review, we update the data on this new drug reported in the literature. There is evidence suggesting that GEMSP is a good candidate for the treatment of multiple sclerosis (MS), an inflammatory an Read More

The most practical synthetic routes to the preparation of as important pharmaceuticals as oxycodone, naloxone, naltrexone, nalbuphine and buprenorphine have utilized the alkaloid, thebaine, as a starting material. This review intends to focus on chemical transformations of morphinans which resulted in morphinandiene derivatives with well-established and novel pharmacological potencies. These chemical transformatio Read More

Quantitative Structure Activity Relationship (QSAR) is an approach of mapping chemical structure to properties. A significant development can be observed in the last two decades in this method which originated from the Hansch analysis based on the logP data and Hammett constant towards a growing importance of the molecular descriptors derived from 3D structure including conformational dynamics and solvation scenario Read More

Thyroid hormone receptors (TRs) exert profound effects on development, metabolism, and multiple specific organ functions. Principally by regulating crucial genes in a variety of tissues, the thyroid hormones, 3,5,3'-triiodo-Lthyronine (L-T3, 1) and 3,5,3',5'-tetraiodo-L-thyronine (L-T4, 2), influence basal calorigenesis and oxygen consumption, cardiac rate and contractility, lipid metabolism, bone structure and strength, and Read More

The anthracycline doxorubicin (DOX) is widely used in chemotherapy due to its efficacy in fighting a wide range of cancers such as carcinomas, sarcomas and hematological cancers. Despite extensive clinical utilization, the mechanisms of action of DOX remain under intense debate. A growing body of evidence supports the view that this drug can be a double-edge sword. Indeed, injury to nontargeted tissues often com Read More

Chagas disease is one of the most important parasitic diseases in Latin America, affecting16 to 18 million people. Nifurtimox and Benznidazol are drugs that are commonly used in its treatment; however, these drugs produce several adverse reactions and are not effective in the chronic phase of the disease. Therefore, the design, synthesis, and biological evaluation of new compounds with potential activity against Trypanozom Read More

The Na+/Ca2+ exchanger (NCX) has a pivotal role in cardiac Na+ and Ca2+ homeostasis and is an essential pathway for Ca2+ extrusion from cardiomyocytes. Altered NCX function may result in abnormal Ca2+ release from the sarcoplasmic reticulum (SR) and impaired cardiac electrical activity and contractility in several diseases, like arrhythmias, ischemia/reperfusion injury, hypertrophy and heart failure. This review foc Read More

Pleiotrophin (PTN) is a recently discovered cytokine which has been found highly upregulated in the substantia nigra and striatum of rodents in experimental models of Parkinson's disease. Interestingly, immunohistochemical studies have shown increased levels of PTN expression in the substantia nigra of patients with Parkinson's disease. Since, in other contexts, PTN has been shown to be critical in repair processes in th Read More