Current Medicinal Chemistry - Volume 13, Issue 2, 2006

Leukotrienes play an important role in the inflammatory process accompanying allergic diseases of respiratory, gastrointestinal and dermatological systems. Leukotrienes are generated from arachidonic acid as a result of the 5-lipoxygenase action. This paper deals with 5-lipoxygenase action mechanism and the following biosynthesis of all leukotrienes. In this article, potential antileukotrienic agents are classified according to t Read More

Symmetry plays a crucial role in a variety of biological processes. For instance, many protein receptors, upon activation, dimerize to its active form and subsequently produce its biological action. Hence, there is a renewal of curiosity for the synthesis of dimeric molecules (or bivalent ligands) capable, not only to interact with specific biologic receptors, but also to induce greater biological responses than the corresponding mon Read More

The proteasome recently gained an exceptional attention as a novel drug target, therefore its inhibitors became important subjects for rational drug design. A synthetic competitive inhibitor Velcade was lately approved in a fast-track process to treat multiple myeloma and is tested with other types of cancers. The proteasome is a major proteolytic assembly in eukaryotic cells responsible for the degradation of most intracellula Read More

In this article we provide an overview on the medicinal chemistry of new bioactive N-acylhydrazone (NAH) derivatives designed through the structural optimization of N-arylhydrazone precursors, originally planned by molecular hybridization of two known 5-lipoxygenase inhibitors, i.e. CBS-1108 and BW-755c. The analgesic, antiedematogenic and platelet anti-aggregating profile of several isosteric NAH compounds was Read More

Prenyloxycoumarins and prenyloxyfuranocoumarins (isopentenyloxy-, geranyloxy-, linear and cyclic sesquiterpenyloxy compounds and their biosynthetic derivatives) represent a family of secondary metabolites that have been considered for years just as intermediates of other coumarin-based compounds. Only in the last two decades these secondary metabolites have been recognized as interesting and valuable biologic Read More

The solubility of drugs and drug-like compounds has been the subject of extensive studies aimed at finding a way to predict solubility from molecular structure. The aqueous solubility of a drug is an important factor that influences its absorption, distribution and elimination in the body. Poor aqueous solubility often causes a drug to appear inactive and may cause other biological problems. Compound solubility in DMSO r Read More