The endocannabinoid system (ECS) is becoming a hot issue of the pharmacology research due to its potential to regulate many physiological and cognitive processes. This paper is a brief overview of the system and of the compounds affecting it as agonists (phytocannabinoids, synthetic cannabinoids, endocannabinoids) or antagonists. Possible utilization of compounds leading to higher levels of endocannabinoids (inhibitors of reuptake/transport of endocannabinoids, inhibitors of Fatty Acid Amide Hydrolase – FAAH, inhibitors of Monoacylglycerol Lipase – MAGL), is also covered.
Chloroquine is a well-established antimalarial medication. This medicine and its analog hydroxychloroquine have appeared as an effective treatment of coronavirus Covid-19 infection. The article reviewed selected aspects of chloroquine in the history of medicinal chemistry, as well as some latest results.
- Klíčová slova
- remdesivir,
- MeSH
- antimalarika MeSH
- chlorochin analýza farmakologie izolace a purifikace terapeutické užití MeSH
Serendipity is still one of the factors involved in drug discovery. Historically it has played a role in the discovery of a range of drugs that have had a great impact on the human therapy. This review presents 20 case studies of such serendipitous drug discoveries selected either for their importance in therapy or other interesting features. Of course, the selection is strictly subjective and many other examples could be added.
All over the world, high drug prices prevent some people to be adequately treated. The price is caused, at least in part, by the complexity of the current drugs and high costs of their discovery and development. The present article reviews some possibilities how to reduce the cost by developing me-too drugs, using repurposing strategy and, last but not least, by generic substitution. The main part of the article deals with the Four Thieves Vinegar initiative offering information necessary for production of Do-It-Yourself (DIY) medicines. All drawbacks of the strategy are discussed.
- Klíčová slova
- domácí výroba léčiv,
- MeSH
- lidé MeSH
- náklady na léky MeSH
- padělané léky MeSH
- příprava léků * MeSH
- Check Tag
- lidé MeSH
The article's aim is to describe to the general chemical audience how results of metabolic studies together with application of kinetic isotope effect of deuterated analogs can lead to a new class of drugs deuterated drugs. The fact is illustrated by several case studies of deuterated analogs of well-known drugs which are currently under development.
- Publikační typ
- abstrakt z konference MeSH
The compound originally known as TIC10 or ONC201 is a new anticancer drug developed by Oncoceutics, Inc. The agent's Investigational New Drug Application for phase I/II clinical studies has been recently approved by Food & Drug Administration. However, a Scripp Institute's group revealed that the compound structure given in all documents, including patents, was erroneous and applied for a patent protection for the correct structure. Chemistry backgrounds associated with this case is reviewed together with the relevant consequences regarding the intellectual property issue.
- Klíčová slova
- bosutinib,
- MeSH
- antitumorózní látky farmakokinetika chemie zásobování a distribuce MeSH
- apoptóza MeSH
- chemické techniky analytické metody využití MeSH
- duševní vlastnictví * MeSH
- farmaceutická technologie MeSH
- isomerie * MeSH
- krystalografie rentgenová MeSH
- kvantitativní vztahy mezi strukturou a aktivitou MeSH
- lidé MeSH
- magnetická rezonanční tomografie MeSH
- příprava léků MeSH
- protein TRAIL MeSH
- tyrosinkinasy * antagonisté a inhibitory chemie MeSH
- Check Tag
- lidé MeSH
- MeSH
- inhibitory fosfodiesteras aplikace a dávkování terapeutické užití MeSH
- inhibitory vychytávání dopaminu aplikace a dávkování terapeutické užití MeSH
- lidé MeSH
- off-label použití léčivého přípravku * dějiny ekonomika MeSH
- sulfonamidy aplikace a dávkování terapeutické užití MeSH
- Check Tag
- lidé MeSH
