Current Medicinal Chemistry - Volume 9, Issue 12, 2002

Resistance to antibiotics is currently a major health concern in treating infectious diseases. The most common mechanism of resistance to β-lactam antibiotics is the production of β-lactamases, which destroy β-lactam antibiotics before they reach the bacterial target. Combination therapy, which involves treatment with a β-lactam antibiotic and a β-lactamase inhibitor, has been successfully used to control resistance during last tw Read More

Modification of cysteine (Cys) residues in proteins, due to (i) the participation of the thiol moiety of this amino acid in oxido-reductions reactions (ii) its ability to strongly coordinate transition metal ions or (iii) its nucleophilic nature and facile reaction with electrophiles, may be of critical importance for the design of novel types of pharmacological agents. Application of such procedures, recently led to the design of novel Read More

Serotonin N-acetyltransferase (arylalkylamine N-acetyltransferase, AANAT) catalyzes the rate-limiting step in the biosynthesis of the circadian hormone melatonin from serotonin. Although melatonin was identified 40 years ago, relatively little is known about its (patho)physiological roles, and a solid scientific foundation is still lacking for most therapeutic applications currently claimed for melatonin. The development of pot Read More

Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a targeting carrier system (alendronate, pamitronate).

The search for pharmacological approaches to neoplastic disease has made some impressive gains started after 1940 when the antileukemic activity of nitrogen mustard was discovered during world war II. It is generally accepted that neoplastic transformation is related to genes alteration or oncogene activation, so the progress in the development of the new drugs for treatment of malignant diseases has been rapid, both i Read More