Mini Reviews in Medicinal Chemistry - Volume 7, Issue 4, 2007

Microwave irradiation has been used to enhance organic reactions since the mid 80's, its use within the field of medicinal chemistry is not so widely evident in the literature. The present review highlights the use of microwave chemistry as an important tool for the fast development of structure activity relationship in several programs related to various therapeutic areas.

Sphingolipids comprise a family of bioactive lipids that exert antagonizing roles in diverse cellular functions such as cell proliferation, growth arrest or apoptosis. Synthesized in the ER/Golgi, sphingolipids are subsequently distributed to different compartments, most predominantly in the plasma membrane, where they integrate signaling platforms. In addition to its precursor role in the synthesis of complex glycosphingolipids, cer Read More

Fondaparinux is a synthetic, five-saccharide chain, AT-dependent, anti-FXa agent. Studies showed that fondaparinux acts in prevention and treatment of venous thromboembolism and in ischemic heart disease, without significant bleeding risk. The drug inhibits thrombin generation, has long half-life and can be administered once-daily without laboratory monitoring. It may be used in HIT treatment.

The development of resistance by the antibiotics in the Gram-positive pathogenic bacteria over the last twenty years and continuing today has created a need for new antibiotic classes, which may be unaffected by existing bacterial resistance. The oxazolidin-2-ones represent not only a new class with a novel mechanism of action, but also satisfy the requirement for overcoming the resistance mechanisms. Both linezolid and Read More

Artemisinin and its synthetic derivatives are widely used for antimalarial agents in the world. Moreover, they are discovered to additionally use as anticancer, antiangiogenesis, antiviral, immunosuppressive, and antifungal agents. Recent research results supported that it is a very promising field in drug discovery. In this review, it will discuss the structural and biological features of artemisinin and its derivatives that have publi Read More

For almost half a century immunologists have tried to tear down the MHC barrier, which separates two unrelated individuals during transplantation. Latest experimental data suggest that a breakthrough in vitro is imminent. Dendritic cells (DCs),which activate naive allo-reactive T-cells (TCs), play a central role in the establishment of allo-antigenspecific immunity. Allograft solid organ rejection is initiated at the foreign endothelial c Read More

New drugs are introduced to the market every year and each individual drug represents a privileged structure for its biological target. In addition, these new chemical entities (NCEs) not only provide insights into molecular recognition, but also serve as drug-like leads for designing future new drugs. To these ends, this review covers the syntheses of 22 NCEs marketed in 2005.