Current Medicinal Chemistry - Volume 13, Issue 30, 2006

This review summarizes the current tendencies observed in the past 5 years in the development of A1 and A2A adenosine receptor antagonists performed in various academia and industry. A1 and A2A AR antagonists are as well xanthines as heteroaromatic derivatives and are most commonly 6:5 fused heteroatomic compounds. Among xanthine-based compounds, some common features could be pointed out. The r Read More

Peptidomimetics have found wide application as bioavailable, biostable, and potent mimetics of naturally occurring biologically active peptides. L-Arginine is a guanidino group-containing basic amino acid, which is positively charged at neutral pH and is involved in many important physiological and pathophysiological processes. Many enzymes display a preference for the arginine residue that is found in many natural substrates Read More

Morbidity and mortality of chronic liver disease are primarily caused by liver cirrhosis and portal hypertension, both of them secondary disorders of progressive liver fibrosis. The main fibrogenic cell type in the liver, the hepatic stellate cell (HSC), is activated and stimulated by several factors, among which the renin-angiotensin-aldosterone system (RAAS) plays a major role. Angiotensin II induces various profibrotic pathways vi Read More

Eight novel 2-(2'-cyclopentyl)- and 2-(2'-cyclohexyl) substituted 1-naphthol derivatives were synthesized in good yield starting from 1-hydroxy-2-naphthoic acid. Two of them, 2-((1- (hydroxymethyl)cyclopentyl)methyl)naphthalene-1-ol (8) and 2-((1-(hydroxymethyl)cyclohexyl)methyl)- naphthalene-1-ol (9) showed anticyclooxygenase activity on COX-2 with IC50 values of 19.90 μM and 7.77 μM, respectively and 9 also inh Read More

Phosphonated nucleosides represent a promising alternative in the improvement of the biological activity of nucleoside analogues in antiviral and anticancer chemotherapy. The basic concept, the chemistry, the different structural modifications and their effects on the antiviral potency will be discussed in this review.

The new generation of biologically active compounds developed during the 20th century relied on knowledge of enzymology and protein structure, and were based initially, on the understanding that proteinprotein and small molecule-protein interactions occurred through a lock-and-key mechanism. Later, evidence suggested that this mechanism was usually followed by a conformational change, known as induced fit. Rec Read More

Parkinson's disease (PD) is a slowly progressive neurodegenerative disorder with a heterogeneous clinical picture and a variable rate of progression. PD is characterized by degeneration of the pigmented neuromelanin bearing cells of the pars compacta of the substantia nigra that leads to a severe dopaminergic denervation of the striatum. Current treatments for PD rely on dopamine replacement therapy, most co Read More

S-100 protein, described initially by Moore, constitutes a large family of at least 20 proteins with calcium binding ability. It is found as homo- or hetero-dimers of two different subunits (A and B). Types S-100AB and S-100BB are described as S-100B protein and are shown to be highly specific for nervous tissue. It is present in the cytosol of glial and Schwann cells, and also in adipocytes and chondrocytes, although in very low c Read More