Medicinal Chemistry Reviews - Online (Discontinued) - Volume 2, Issue 3, 2005

With the use of chlorpromazine and other traditional antipsychotics for psychosis, it was soon discovered that the antipsychotic efficacy of this class of medications was closely associated with their ability to block dopamine D2 receptors in the brain. This prompted the hypothesis that the etiology of schizophrenia and other psychotic illnesses might be caused by a dysregulation of dopamine. This hypothesis, that the dopamine syst Read More

Carbapenem-hydrolyzing β-lactamases of several Ambler molecular classes have been reported as the source of acquired β-lactam antibiotic resistance in Gram negative bacteria. The metallo-enzymes of Ambler class B are the most prevalent enzymes in this case. These clavulanic-acid resistant enzymes have a large spectrum of hydrolysis including penicillins, cephalosporins (third and fourth generations), carbapenems Read More

The constant increase of life expectancy is associated with major aging of developed populations. This indicates that the new century will have one of most epidemic progressions of cardiovascular, cancer and inflammatory diseases. The high challenge for medical research is to compress such morbidity. Invertebrates have demonstrated to be truly useful models in drug discovery for such aging diseases. The last decade, drug d Read More

The production, under environmentally benign conditions, of efficient and more cost-effective anti-infective agents (available to the whole mankind) is one of most ambitious dreams of the industrial medicinal chemistry. Semi-synthetic βlactam antibiotics are very effective anti-infective agents. They are very stable and can be used via oral delivery. They exhibit a very wide spectrum of anti-bacterial activity and minimal side effe Read More

Techniques of the phage display libraries construction have been dramatically improved. This allowed researchers to expand the application field to cancer biology. Tumor targeting -selective delivery of active compounds to the tumor sites for cancer imaging or treatment presents obvious advantages as compared to chemotherapeutic approachkilling rapidly proliferating cells. Tumor-avid peptides can be efficiently identifie Read More

Parasitic protozoa of the genus Leishmania infect mammalian mononuclear phagocytic cells causing a potentially fatal disease with a broad spectrum of clinical manifestations. The drugs of choice used in the leishmaniasis therapy are significantly toxic, expensive and faced with a growing frequency of refractory infections. Thus the search for new leishmanicidal compounds is urgently required. In order to perform Read More

Ligands of the benzodiazepine binding site of the GABAA receptor come in three flavors: positive allosteric modulators, negative allosteric modulators and antagonists all of which can bind with high affinity. The GABAA receptor is a pentameric protein which forms a chloride selective ion channel and ligands of the benzodiazepine binding site stabilize three different conformations of this protein. Classical benzodiazepines e Read More

In the multi-cause and multi-step diseases we globally refer to as cancer, often the same or redundant biochemical circuits are disrupted or uncoupled by the cumulative action of diverse mutation events. Anticancer agents have been extensively designed and selected by their ability to specifically interact with malignant cells by the targeting of proteins, mRNAs or DNA sequences involved in the production of a transfor Read More