The group of researchers, including chemists from the University of Silesia, developed two new carbamate derivatives. These substances may find application in pharmaceuticals used to reduce symptoms of Alzheimer’s disease.
The protein called amyloid beta accumulates in the brain of a diseased person in the form of senile plaques. They create deposits leading to gradual loss of neurons and synapses in the cerebral cortex, which as a result lowers diseased person’s intellectual efficiency. The disease ends with the death of a patient. Right now its treatment mostly consists in alleviation of the symptoms. Provision of care for people suffering from Alzheimer’s disease constitutes an economic and social challenge for the modern world.
The drugs prescribed now contain mostly enzymes responsible for regulating breakdown of acetylcholine. The drugs block this breakdown, which results in rise of the neurotransmitter’s level in a patient’s brain. This in turn compensates for its decreased concentration due to the death of cholinergic neurons. The substances that can block the said breakdown include, among others, organic compounds called carbamate.
By modifying their structure we can obtain a selective or non-selective substance that has an effect on some enzymes. This is important, because depending on the stage of Alzheimer’s disease, the concentration of enzymes responsible for the said breakdown of acetylcholine is changing. Only three medical substances are available in the therapy at the initial and intermediate stage of the disease. They are characterized by low bioavailability, low permeability of blood-brain barrier and may cause numerous undesirable side effects. Moreover, there is a need on the pharmaceutical market for the compounds which will regulate breakdown of acetylcholine at the advanced stage of the disease.
New carbamate derivatives were obtained by the researchers from Poland, Czech Republic and Slovakia. Ultimately these compounds will be studied as active substances intended to alleviate symptoms of Alzheimer’s disease, owing to their effect on the enzymes responsible for regulating breakdown of acetylcholine both at the initial and advanced stage of the disease.
New carbamate derivatives and their application have been patented. The authors of these solutions are: Dariusz Kozakiewicz MSc, Prof. Jarosław Polański from the Institute of Chemistry at the University of Silesia and Prof. Josef Jampilek from Comenius University in Bratislava (Slovakia), Ales Imramowsky and Šárka Štěpánková from University of Pardubice (the Czech Republic).