Current Medicinal Chemistry - Volume 11, Issue 19, 2004

The discovery and development of novel drugs has been influenced over the last several decades by new techniques in medicinal chemistry. Combinatorial and parallel synthesis chemistry techniques have opened up immense opportunities in drug discovery and development efforts. These techniques, which include solid phase organic synthesis and polymer-assisted synthesis in solution, have been routinely applied to Read More

The search for an ideal anticoagulant has spanned decades and has resulted in several approaches and the identification of novel target molecules for preventing and treating thrombosis. The first group of new anticoagulant agents acting through direct inhibition of coagulation factors were inhibitors of thrombin, but factor Xa inhibitors and, most recently, factor VIIa inhibitors have become attractive candidates. The structur Read More

Purine bases and their bioisosteric analogs are widely used as building blocks in combinatorial chemistry. Recently a great number of fused pyrimidine derivatives became known as potential drug molecules against various types of proliferative diseases, caused by over-expression of protein kinases [1]. One of the most important compound families are quinazolines : e.g. the best inhibitor of EGFR tyrosine kinase is PD Read More

The permanent therapeutic importance of morphine derivatives in pain treatment has inspired continual synthetic efforts to modify the rigid pentacyclic systems in search for new selective analgesic agents. As a result, several morphinane oximes have been synthesized recently, which have the additional advantage of possessing an oxime group that can provide a method for selective determination of opiate alkaloids i Read More

Structural diversity of carbohydrates plays a crucial role in their large variety of roles in biological systems. This paper focuses on aspects of structure and biological functions of three classes of carbohydrates, N-linked oligosaccharides, blood group oligosaccharides and glycosaminoglycans. Conformations and dynamics in solution, as well as structure of protein-carbohydrate complexes are discussed. A s Read More

The classical 4'-oxonucleoside analogs exhibit interesting biological activities such as antibiotic, antiviral and antitumor, which are believed to be the result of inhibition of the viral or cellular DNA or RNA polymerase after being converted to their corresponding 5'-triphosphates. However, the activity of 4'- oxonucleosides were limited by their susceptibility to degradation by nucleoside phosphorylases or acid hydrolysis. This asp Read More

New drugs are urgently required for Human African Trypanosomiasis (sleeping sickness), a disease which has re-emerged as a major health threat in Sub-Saharan Africa. The third enzyme of the pentose phosphate pathway, 6-phosphogluconate dehydrogenase, has been shown to be a good target for drugs. The enzyme is essential to the trypanosomes that causes sleeping sickness and structural differences when compared Read More