Mini Reviews in Medicinal Chemistry - Volume 10, Issue 4, 2010

The rapid emergence of drug resistance intensified the search for new antimicrobial agents, leading to lots of novel derivatives obtained from 14- and 15-membered macrolides by chemical modifications. Many of them exhibited enhanced antibacterial activity and expanded antibacterial spectrum. Especially some of them were found to be potent for the treatment of multi-drug-resistant bacterial infections. Besides, the o Read More

Since most of the proteinogenic α-amino acids contain a chiral carbon atom, the stereoisomers of both these amino acids and the peptides in which they are to be found may possess differences in biological activity in living systems. The important analytical task of the separation of optical isomers is achieved mainly by chromatographic methods. This special review surveys direct and indirect HPLC separations of biologically Read More

The aim of this review is to summarize the most comprehensive results in the field of bis-aromatic compounds targeting DNA and RNA, whereby both aromatic units of small molecule bind to the polynucleotide by the aromatic stacking interactions. The most recent results about structure - DNA/RNA binding affinity, selectivity and biological implications are discussed for bis-intercalators, sterically restricted macrocyclic and t Read More

Although the halogen bond has attracted much interest in chemistry and material science communities, its implications for drug design are just now coming to light. The protein-ligand interactions through short halogen— oxygen/nitrogen/sulfur contacts have been observed in crystal structures for a long time, but only in recent years, with the experimental and theoretical progress in weak biological interactions, espec Read More

The inhibition of α-glucosidase and α-amylase, enzymes involved in the digestion of carbohydrates, can significantly reduce the post-prandial increase of blood glucose and therefore can be an important strategy in the management of blood glucose level in type 2 diabetic and borderline patients. Currently, there is renewed interest in plant-based medicines and functional foods modulating physiological effects in the preve Read More

Photodynamic therapy (PDT) is a versatile methodology to treat various diseases but the drugs (photosensitizers) specifically aimed at individual character of diseases are urgently needed. Among those, the perilenoquinoid photosensitizers were thought of low PDT effectiveness to solid tumors due to low absorption on the “photodynamic window” but may be specially suitable for PDT to some microvascular diseases, suc Read More

The antioxidant enzymes, such as superoxide dismutase, catalase, glutathione peroxidase, and glutathione S-transferase contribute dominatingly to enhance cellular antioxidant defense against oxidative stress. They act cooperatively to scavenge reactive oxygen species, and not one of them can singlehandedly clear all forms of reactive oxygen species. On the basis of the structural understanding for these natural enzymes, Read More