Current Bioactive Compounds - Volume 5, Issue 2, 2009

This issue is aimed for anyone who is interested or works with current theoretical methods in medicinal chemistry, with particular interest in chemoinformatics and bioinformatics for many therapeutic purposes. This issue attempts to convey something of the fascination of working in the multidisciplinar field of Medicinal Chemistry, which overlap knowledge of chemistry, physics, biochemistry, biology and pharmacology. Al Read More

α- and β-glucosidases are postulated to be a very attractive therapeutic target since they catalyze the cleavage of glycosidic bonds releasing glucose from the non-reducing end of an oligo- or polysaccharide chain involved in glycoprotein biosynthesis. Glucosidase inhibitors are currently of interest owing to their promising therapeutic potential in the treatment of disorders such as diabetes, AIDS, metastatic cancer and lysos Read More

The high frequency of contamination by herbicides suggests the need for more active and selective herbicides. Glyphosate is the active component of one of the top-selling herbicides, which is also a potent EPSP synthase inhibitor. That is a key enzyme in the shikimic acid pathway, which is found only in plants and some microorganisms. Thus, EPSP synthase is regarded as a prime target for herbicides. In this line, molecular modeli Read More

Alzheimer's disease has become one of the most serious healthcare problems nowadays, where age is clearly the major risk factor. The pathology of the disease is characterized by the formation of senile plaques outside the neurons, which are composed, predominantly, by the β-amyloid (Aβ) peptide. Considering that β-secretase is an aspartyl protease involved in the cleavage of the amyloid precursor, the first step required fo Read More

The enzyme reverse transcriptase (RT) is essential in the replication of human immunodeficiency virus (HIV). Non-nucleoside reverse transcriptase inhibitors or NNRTI's are a promising class of anti-HIV drugs, which block the chemical step of DNA polymerization reaction by binding at the allosteric site of RT, leading to a viral suppression. A major limitation to the success of therapy with NNRTIs is the rapid development of d Read More

Tuberculosis (TB) remains one of the most deadly infectious diseases in the world, killing about 2 million people per year, and mostly affecting the world's poorest population. The length of current regimens for treatment of TB is long (6-9 months) with a high pill burden. Furthermore, one third of the world population is infected, though asymptomatically, with latent TB and is at risk of developing active TB disease during their lif Read More

Searching for bioactive molecules from natural source represents an attractive strategy. Natural bioactive molecules form the backbone of modern therapeutics. For that reason the glycolipoprotein extract (G-90) from tissue homogenate of earthworm Eisenia foetida represents a valuable source of bioactive molecules. The molecules in this preparation exhibit many biological characteristics, useful in different biological pro Read More

Betulinic acid, a naturally occurring pentacyclic triterpenoid was found in many plants. It has been isolated with considerable success from birch bark. Apart from its isolation from plants, betulinic acid is also synthesized from betulin by different methods. It exhibits broad range of biological activities such as anticancer, antimalarial, anti-HIV, antiviral and immunomodulator activity. Anticancer property of this molecule is attri Read More