The process of developing a suitable active ingredient with the desired properties is a
financially and time-consuming process. Industry research begins with high-throughput
screening to arrive at lead compounds. A lead compound is a natural, semi-synthetic or
synthetic compound with pharmacological and biological activity. Lead compounds are similar
to each other, but slightly differ in structure, physico-chemical properties, efficiency of action,
affinity to the target, and the like. In the master's thesis, we mainly focused on the solubility
and metabolism aspects of these lead compounds, which will give us a better insight into the
relevance of the synthesized compound as a potential medicinal agent. Through the solubility
and metabolism parameters of lead compounds, we can roughly conclude whether this
compound has potential and whether it is suitable for more detailed research. Solubility and
metabolism were demonstrated using the analytical method of high-resolution liquid
chromatography on a Thermo-Fischer UPLC system in the premises of the Faculty of
Pharmacy. To evaluate solubility, we have used a seven-point calibration curve to cover as
large a concentration range as possible in which we could claim the precision and accuracy of
the results. In metabolism, in addition to the lead compound, we also performed a parallel test
of testosterone metabolism daily, which served as a control for the adequacy of the procedure
and a tool with which we could evaluate the results of the metabolic stability of lead
compounds. We found that the tested compounds are relatively poorly soluble, but
metabolically stable, which will enable the design of new analogues of these compounds with
improved properties.
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