Coumarins are natural products characterized as 2H-chromen-2-one, according to IUPAC nomenclature, largely distributed in plants, as well as, in species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert non-covalent interactions with many enzymes and receptors in living organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarin compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, anti-diabetics, anti-inflammatory, antibacterial, antifungal, and anti-neurodegenerative agents. Thus, this work aims at contributing to the development of new rational research projects searching for new treatments and bioactive compounds for many pathologies using coumarin derivatives.

A synthetic procedure for obtaining the fluorescent coumarin umbelliferone (7-hydroxycoumarin) and its spectral parameters were fully developed aiming at an undergraduate organic chemistry laboratory class. Umbelliferone is traditionally prepared via Pechmann condensation using malic acid, resorcinol and sulfuric acid as catalyst. The use of domestic microwave oven and the absence of solvent allow our methodology to be simple, fast and easy applied in obtaining umbelliferone at organic chemistry laboratory being greener than classical techniques of synthesis. In this class the student will learn how to measure the potency of a microwave oven, the applicability of this kind of irradiation in the organic synthesis of fluorescent compounds and how to determine the pKa of an organic compound through an UV/VIS spectrometric analysis. These experiments were designed to be suitable for a second and third year undergraduate curriculum.

In the 21st century, medicinal chemists will face many challenges to improve the quality of life of populations. The challenges consist of emerging infectious (ex. bacterial, viral and parasite infections) and non-communicable diseases (ex. autoimmune, Alzheimer disease, Parkinson’s disease) that will require innovative technologies (ex. microfluidics, nanotechnology, biotechnology) to be fully understood and combated. In this work, we indicate trends, perspectives and opportunities related to drug discovery as well as highlight the tools and strategies that could be used in drug discovery of the 21st century.

ABSTRACT New acylhydrazone-based palladacycles are prepared and evaluated as pre-catalysts in Mirozoki-Heck and oxyarylation reactions.

Medicinal Chemistry includes the invention, discovery, design, identification, and interpretation of the molecular mechanism of action of biologically active compounds. In addition to the discovery of bioactive molecules, Medicinal Chemistry investigates drug metabolism and the relationships between chemical structure and biological activity. The advances achieved in the 20th century have significantly contributed to the better understanding of pathophysiological processes as well as the development of new, safer and more effective drugs for many diseases. In this article, we review the evolution of Medicinal Chemistry in Brazil during the last 40 years and evaluate the impact of the Brazilian contributions in the international context. The analyzed data revealed that Medicinal Chemistry research in Brazil has increased exponentially in the last two decades, the research groups became more well-distributed across the Brazilian regions and our scientific contributions have significant impact in the main journals of the field. Therefore, aiming at evolving steadily and striving for excellence in drug discovery and development, we shall focus on national and international collaborations and investment in translational research, as well.